gonadotropin-releasing hormone receptor isoform 1 [Homo sapiens]
Protein Classification
G protein-coupled receptor family protein( domain architecture ID 705710)
G protein-coupled receptor family protein is a seven-transmembrane G protein-coupled receptor (7TM-GPCR) family protein which typically transmits an extracellular signal into the cell by the conformational rearrangement of the 7TM helices and by the subsequent binding and activation of an intracellular heterotrimeric G protein; GPCR ligands include light-sensitive compounds, odors, pheromones, hormones, and neurotransmitters
List of domain hits
| Name | Accession | Description | Interval | E-value | |||||
| 7tm_GPCRs super family | cl28897 | seven-transmembrane G protein-coupled receptor superfamily; This hierarchical evolutionary ... |
36-328 | 8.18e-119 | |||||
seven-transmembrane G protein-coupled receptor superfamily; This hierarchical evolutionary model represents the seven-transmembrane (7TM) receptors, often referred to as G protein-coupled receptors (GPCRs), which transmit physiological signals from the outside of the cell to the inside via G proteins. GPCRs constitute the largest known superfamily of transmembrane receptors across the three kingdoms of life that respond to a wide variety of extracellular stimuli including peptides, lipids, neurotransmitters, amino acids, hormones, and sensory stimuli such as light, smell and taste. All GPCRs share a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. However, some 7TM receptors, such as the type 1 microbial rhodopsins, do not activate G proteins. Based on sequence similarity, GPCRs can be divided into six major classes: class A (the rhodopsin-like family), class B (the Methuselah-like, adhesion and secretin-like receptor family), class C (the metabotropic glutamate receptor family), class D (the fungal mating pheromone receptors), class E (the cAMP receptor family), and class F (the frizzled/smoothened receptor family). Nearly 800 human GPCR genes have been identified and are involved essentially in all major physiological processes. Approximately 40% of clinically marketed drugs mediate their effects through modulation of GPCR function for the treatment of a variety of human diseases including bacterial infections. The actual alignment was detected with superfamily member cd15383: Pssm-ID: 475119 [Multi-domain] Cd Length: 295 Bit Score: 343.97 E-value: 8.18e-119
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| Name | Accession | Description | Interval | E-value | |||||
| 7tmA_GnRHR_vertebrate | cd15383 | vertebrate gonadotropin-releasing hormone receptors, member of the class A family of ... |
36-328 | 8.18e-119 | |||||
vertebrate gonadotropin-releasing hormone receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; GnRHR, also known as luteinizing hormone releasing hormone receptor (LHRHR), plays an central role in vertebrate reproductive function; its activation by binding to GnRH leads to the release of follicle stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary gland. GnRHR is expressed predominantly in the gonadotrope membrane of the anterior pituitary as well as found in numerous extrapituitary tissues including lymphocytes, breast, ovary, prostate, and cancer cell lines. There are at least two types of GnRH receptors, GnRHR1 and GnRHR2, which couple primarily to G proteins of the Gq/11 family. GnRHR is closely related to the adipokinetic hormone receptor (AKH), which binds to a lipid-mobilizing hormone that is involved in control of insect metabolism. They share a common ancestor and are members of the class A of the seven-transmembrane, G-protein coupled receptor (GPCR) superfamily. Pssm-ID: 320505 [Multi-domain] Cd Length: 295 Bit Score: 343.97 E-value: 8.18e-119
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| 7tm_1 | pfam00001 | 7 transmembrane receptor (rhodopsin family); This family contains, amongst other ... |
76-323 | 4.75e-35 | |||||
7 transmembrane receptor (rhodopsin family); This family contains, amongst other G-protein-coupled receptors (GCPRs), members of the opsin family, which have been considered to be typical members of the rhodopsin superfamily. They share several motifs, mainly the seven transmembrane helices, GCPRs of the rhodopsin superfamily. All opsins bind a chromophore, such as 11-cis-retinal. The function of most opsins other than the photoisomerases is split into two steps: light absorption and G-protein activation. Photoisomerases, on the other hand, are not coupled to G-proteins - they are thought to generate and supply the chromophore that is used by visual opsins. Pssm-ID: 459624 [Multi-domain] Cd Length: 256 Bit Score: 128.18 E-value: 4.75e-35
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| PHA03087 | PHA03087 | G protein-coupled chemokine receptor-like protein; Provisional |
39-327 | 4.96e-14 | |||||
G protein-coupled chemokine receptor-like protein; Provisional Pssm-ID: 222976 [Multi-domain] Cd Length: 335 Bit Score: 71.73 E-value: 4.96e-14
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| Name | Accession | Description | Interval | E-value | |||||
| 7tmA_GnRHR_vertebrate | cd15383 | vertebrate gonadotropin-releasing hormone receptors, member of the class A family of ... |
36-328 | 8.18e-119 | |||||
vertebrate gonadotropin-releasing hormone receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; GnRHR, also known as luteinizing hormone releasing hormone receptor (LHRHR), plays an central role in vertebrate reproductive function; its activation by binding to GnRH leads to the release of follicle stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary gland. GnRHR is expressed predominantly in the gonadotrope membrane of the anterior pituitary as well as found in numerous extrapituitary tissues including lymphocytes, breast, ovary, prostate, and cancer cell lines. There are at least two types of GnRH receptors, GnRHR1 and GnRHR2, which couple primarily to G proteins of the Gq/11 family. GnRHR is closely related to the adipokinetic hormone receptor (AKH), which binds to a lipid-mobilizing hormone that is involved in control of insect metabolism. They share a common ancestor and are members of the class A of the seven-transmembrane, G-protein coupled receptor (GPCR) superfamily. Pssm-ID: 320505 [Multi-domain] Cd Length: 295 Bit Score: 343.97 E-value: 8.18e-119
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| 7tmA_GnRHR-like | cd15195 | gonadotropin-releasing hormone and adipokinetic hormone receptors, member of the class A ... |
36-326 | 5.24e-85 | |||||
gonadotropin-releasing hormone and adipokinetic hormone receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Gonadotropin-releasing hormone (GnRH) and adipokinetic hormone (AKH) receptors share strong sequence homology to each other, suggesting that they have a common evolutionary origin. GnRHR, also known as luteinizing hormone releasing hormone receptor (LHRHR), plays an central role in vertebrate reproductive function; its activation by binding to GnRH leads to the release of follicle stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary gland. Adipokinetic hormone (AKH) is a lipid-mobilizing hormone that is involved in control of insect metabolism. Generally, AKH behaves as a typical stress hormone by mobilizing lipids, carbohydrates and/or certain amino acids such as proline. Thus, it utilizes the body's energy reserves to fight the immediate stress problems and subdue processes that are less important. Although AKH is known to responsible for regulating the energy metabolism during insect flying, it is also found in insects that have lost its functional wings and predominantly walk for their locomotion. Both GnRH and AKH receptors are members of the class A of the seven-transmembrane, G-protein coupled receptor (GPCR) superfamily. Pssm-ID: 320323 [Multi-domain] Cd Length: 293 Bit Score: 258.10 E-value: 5.24e-85
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| 7tmA_AKHR | cd15382 | adipokinetic hormone receptor, member of the class A family of seven-transmembrane G ... |
45-328 | 3.62e-69 | |||||
adipokinetic hormone receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; Adipokinetic hormone (AKH) is a lipid-mobilizing hormone that is involved in control of insect metabolism. Generally, AKH behaves as a typical stress hormone by mobilizing lipids, carbohydrates and/or certain amino acids such as proline. Thus, it utilizes the body's energy reserves to fight the immediate stress problems and subdue processes that are less important. Although AKH is known to responsible for regulating the energy metabolism during insect flight, it is also found in insects that have lost its functional wings and predominantly walk for their locomotion. AKH is structurally related to the mammalian gonadotropin-releasing hormone (GnRH) and they share a common ancestor. Both GnRH and AKH receptors are members of the class A of the seven-transmembrane, G-protein coupled receptor (GPCR) superfamily. Pssm-ID: 320504 [Multi-domain] Cd Length: 298 Bit Score: 217.56 E-value: 3.62e-69
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| 7tmA_GnRHR_invertebrate | cd15384 | invertebrate gonadotropin-releasing hormone receptors, member of the class A family of ... |
37-328 | 2.03e-55 | |||||
invertebrate gonadotropin-releasing hormone receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; GnRHR, also known as luteinizing hormone releasing hormone receptor (LHRHR), plays an central role in vertebrate reproductive function; its activation by binding to GnRH leads to the release of follicle stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary gland. GnRHR is expressed predominantly in the gonadotrope membrane of the anterior pituitary as well as found in numerous extrapituitary tissues including lymphocytes, breast, ovary, prostate, and cancer cell lines. There are at least two types of GnRH receptors, GnRHR1 and GnRHR2, which couple primarily to G proteins of the Gq/11 family. GnRHR is closely related to the adipokinetic hormone receptor (AKH), which binds to a lipid-mobilizing hormone that is involved in control of insect metabolism. They share a common ancestor and are members of the class A of the seven-transmembrane, G-protein coupled receptor (GPCR) superfamily. Pssm-ID: 320506 [Multi-domain] Cd Length: 293 Bit Score: 182.25 E-value: 2.03e-55
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| 7tmA_Vasopressin-like | cd14986 | vasopressin receptors and its related G protein-coupled receptors, member of the class A ... |
36-328 | 4.22e-55 | |||||
vasopressin receptors and its related G protein-coupled receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Members of this group form a subfamily within the class A G-protein coupled receptors (GPCRs), which includes the vasopressin and oxytocin receptors, the gonadotropin-releasing hormone receptors (GnRHRs), the neuropeptide S receptor (NPSR), and orphan GPR150. These receptors share significant sequence homology with each other, suggesting that they have a common evolutionary origin. Vasopressin, also known as arginine vasopressin or anti-diuretic hormone, is a neuropeptide synthesized in the hypothalamus. The actions of vasopressin are mediated by the interaction of this hormone with three tissue-specific subtypes: V1AR, V1BR, and V2R. Although vasopressin differs from oxytocin by only two amino acids, they have divergent physiological functions. Vasopressin is involved in regulating osmotic and cardiovascular homeostasis, whereas oxytocin plays an important role in the uterus during childbirth and in lactation. GnRHR, also known as luteinizing hormone releasing hormone receptor (LHRHR), plays an central role in vertebrate reproductive function; its activation by binding to GnRH leads to the release of follicle stimulating hormone (FSH) and luteinizing hormone (LH) from the pituitary gland. Neuropeptide S (NPS) promotes arousal and anxiolytic-like effects by activating its cognate receptor NPSR. NPSR has also been associated with asthma and allergy. GPR150 is an orphan receptor closely related to the oxytocin and vasopressin receptors. Pssm-ID: 320117 [Multi-domain] Cd Length: 295 Bit Score: 181.42 E-value: 4.22e-55
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| 7tmA_Vasopressin_Oxytocin | cd15196 | vasopressin and oxytocin receptors, member of the class A family of seven-transmembrane G ... |
36-327 | 8.90e-44 | |||||
vasopressin and oxytocin receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Vasopressin (also known as arginine vasopressin or anti-diuretic hormone) and oxytocin are synthesized in the hypothalamus and are released from the posterior pituitary gland. The actions of vasopressin are mediated by the interaction of this hormone with three receptor subtypes: V1aR, V1bR, and V2R. These subtypes are differ in localization, function, and signaling pathways. Activation of V1aR and V1bR stimulate phospholipase C, while activation of V2R stimulates adenylate cyclase. Although vasopressin and oxytocin differ only by two amino acids and stimulate the same cAMP/PKA pathway, they have divergent physiological functions. Vasopressin is involved in regulating blood pressure and the balance of water and sodium ions, whereas oxytocin plays an important role in the uterus during childbirth and in lactation. Pssm-ID: 320324 [Multi-domain] Cd Length: 264 Bit Score: 151.23 E-value: 8.90e-44
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| 7tm_classA_rhodopsin-like | cd00637 | rhodopsin receptor-like class A family of the seven-transmembrane G protein-coupled receptor ... |
78-327 | 2.42e-41 | |||||
rhodopsin receptor-like class A family of the seven-transmembrane G protein-coupled receptor superfamily; Class A rhodopsin-like receptors constitute about 90% of all GPCRs. The class A GPCRs include the light-sensitive rhodopsin as well as receptors for biogenic amines, lipids, nucleotides, odorants, peptide hormones, and a variety of other ligands. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Based on sequence similarity, GPCRs can be divided into six major classes: class A (rhodopsin-like family), class B (Methuselah-like, adhesion and secretin-like receptor family), class C (metabotropic glutamate receptor family), class D (fungal mating pheromone receptors), class E (cAMP receptor family), and class F (frizzled/smoothened receptor family). Nearly 800 human GPCR genes have been identified and are involved essentially in all major physiological processes. Approximately 40% of clinically marketed drugs mediate their effects through modulation of GPCR function for the treatment of a variety of human diseases including bacterial infections. Pssm-ID: 410626 [Multi-domain] Cd Length: 275 Bit Score: 145.12 E-value: 2.42e-41
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| 7tmA_V1aR | cd15385 | vasopressin receptor subtype 1A, member of the class A family of seven-transmembrane G ... |
36-327 | 2.00e-39 | |||||
vasopressin receptor subtype 1A, member of the class A family of seven-transmembrane G protein-coupled receptors; V1a-type receptor is a G(q/11)-coupled receptor that mediates blood vessel constriction. Vasopressin (also known as arginine vasopressin or anti-diuretic hormone) is synthesized in the hypothalamus and is released from the posterior pituitary gland. The actions of vasopressin are mediated by the interaction of this hormone with three receptor subtypes: V1aR, V1bR, and V2R. These subtypes are differ in localization, function, and signaling pathways. Activation of V1aR and V1bR stimulate phospholipase C, while activation of V2R stimulates adenylate cyclase. Although vasopressin and oxytocin differ only by two amino acids and stimulate the same cAMP/PKA pathway, they have divergent physiological functions. Vasopressin is involved in regulating blood pressure and the balance of water and sodium ions, whereas oxytocin plays an important role in the uterus during childbirth and in lactation. Pssm-ID: 320507 [Multi-domain] Cd Length: 301 Bit Score: 140.73 E-value: 2.00e-39
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| 7tmA_CCKR-like | cd14993 | cholecystokinin receptors and related proteins, member of the class A family of ... |
83-327 | 1.98e-37 | |||||
cholecystokinin receptors and related proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This group represents four G-protein coupled receptors that are members of the RFamide receptor family, including cholecystokinin receptors (CCK-AR and CCK-BR), orexin receptors (OXR), neuropeptide FF receptors (NPFFR), and pyroglutamylated RFamide peptide receptor (QRFPR). These RFamide receptors are activated by their endogenous peptide ligands that share a common C-terminal arginine (R) and an amidated phenylanine (F) motif. CCK-AR (type A, alimentary; also known as CCK1R) is found abundantly on pancreatic acinar cells and binds only sulfated CCK-peptides with very high affinity, whereas CCK-BR (type B, brain; also known as CCK2R), the predominant form in the brain and stomach, binds CCK or gastrin and discriminates poorly between sulfated and non-sulfated peptides. CCK is implicated in regulation of digestion, appetite control, and body weight, and is involved in neurogenesis via CCK-AR. There is some evidence to support that CCK and gastrin, via their receptors, are involved in promoting cancer development and progression, acting as growth and invasion factors. Orexins (OXs; also referred to as hypocretins) are neuropeptide hormones that regulate the sleep-wake cycle and potently influence homeostatic systems regulating appetite and feeding behavior or modulating emotional responses such as anxiety or panic. OXs are synthesized as prepro-orexin (PPO) in the hypothalamus and then proteolytically cleaved into two forms of isoforms: orexin-A (OX-A) and orexin-B (OX-B). OXA is a 33 amino-acid peptide with N-terminal pyroglutamyl residue and two intramolecular disulfide bonds, whereas OXB is a 28 amino-acid linear peptide with no disulfide bonds. OX-A binds orexin receptor 1 (OX1R) with high-affinity, but also binds with somewhat low-affinity to OX2R, and signals primarily to Gq coupling, whereas OX-B shows a strong preference for the orexin receptor 2 (OX2R) and signals through Gq or Gi/o coupling. The 26RFa, also known as QRFP (Pyroglutamylated RFamide peptide), is a 26-amino acid residue peptide that exerts similar orexigenic activity including the regulation of feeding behavior in mammals. It is the ligand for G-protein coupled receptor 103 (GPR103), which is predominantly expressed in paraventricular (PVN) and ventromedial (VMH) nuclei of the hypothalamus. GPR103 shares significant protein sequence homology with orexin receptors (OX1R and OX2R), which have recently shown to produce a neuroprotective effect in Alzheimer's disease by forming a functional heterodimer with GPR103. Neuropeptide FF (NPFF) is a mammalian octapeptide that has been implicated in a wide range of physiological functions in the brain including pain sensitivity, insulin release, food intake, memory, blood pressure, and opioid-induced tolerance and hyperalgesia. The effects of NPFF are mediated through neuropeptide FF1 and FF2 receptors (NPFF1-R and NPFF2-R) which are predominantly expressed in the brain. NPFF induces pro-nociceptive effects, mainly through the NPFF1-R, and anti-nociceptive effects, mainly through the NPFF2-R. Pssm-ID: 320124 [Multi-domain] Cd Length: 296 Bit Score: 135.42 E-value: 1.98e-37
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| 7tmA_NPSR | cd15197 | neuropeptide S receptor, member of the class A family of seven-transmembrane G protein-coupled ... |
45-327 | 4.69e-36 | |||||
neuropeptide S receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; Neuropeptide S (NPS) promotes arousal and anxiolytic-like effects by activating its cognate receptor NPSR. NPSR is widely expressed in the brain, and its activation induces an elevation of intracellular calcium and cAMP concentrations, presumably by coupling to G(s) and G(q) proteins. Mutations in NPSR have been associated with an increased susceptibility to asthma. NPSR was originally identified as an orphan receptor GPR154 and is also known as G protein receptor for asthma susceptibility (GPRA) or vasopressin receptor-related receptor 1 (VRR1). Pssm-ID: 320325 [Multi-domain] Cd Length: 294 Bit Score: 131.78 E-value: 4.69e-36
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| 7tm_1 | pfam00001 | 7 transmembrane receptor (rhodopsin family); This family contains, amongst other ... |
76-323 | 4.75e-35 | |||||
7 transmembrane receptor (rhodopsin family); This family contains, amongst other G-protein-coupled receptors (GCPRs), members of the opsin family, which have been considered to be typical members of the rhodopsin superfamily. They share several motifs, mainly the seven transmembrane helices, GCPRs of the rhodopsin superfamily. All opsins bind a chromophore, such as 11-cis-retinal. The function of most opsins other than the photoisomerases is split into two steps: light absorption and G-protein activation. Photoisomerases, on the other hand, are not coupled to G-proteins - they are thought to generate and supply the chromophore that is used by visual opsins. Pssm-ID: 459624 [Multi-domain] Cd Length: 256 Bit Score: 128.18 E-value: 4.75e-35
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| 7tmA_V1bR | cd15386 | vasopressin receptor subtype 1B, member of the class A family of seven-transmembrane G ... |
36-327 | 9.83e-35 | |||||
vasopressin receptor subtype 1B, member of the class A family of seven-transmembrane G protein-coupled receptors; The V1b receptor is specifically expressed in corticotropes of the anterior pituitary and plays a critical role in regulating the activity of hypothalamic-pituitary-adrenal axis, a key part of the neuroendocrine system that controls reactions to stress, by maintaining adrenocorticotropic hormone (ACTH) and corticosterone levels. Vasopressin (also known as arginine vasopressin or anti-diuretic hormone) is synthesized in the hypothalamus and is released from the posterior pituitary gland. The actions of vasopressin are mediated by the interaction of this hormone with three receptor subtypes: V1aR, V1bR, and V2R. These subtypes are differ in localization, function, and signaling pathways. Activation of V1aR and V1bR stimulate phospholipase C, while activation of V2R stimulates adenylate cyclase. Although vasopressin and oxytocin differ only by two amino acids and stimulate the same cAMP/PKA pathway, they have divergent physiological functions. Vasopressin is involved in regulating blood pressure and the balance of water and sodium ions, whereas oxytocin plays an important role in the uterus during childbirth and in lactation. Pssm-ID: 320508 [Multi-domain] Cd Length: 302 Bit Score: 128.38 E-value: 9.83e-35
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| 7tmA_V2R | cd15388 | vasopressin receptor 2, member of the class A family of seven-transmembrane G protein-coupled ... |
36-327 | 6.99e-33 | |||||
vasopressin receptor 2, member of the class A family of seven-transmembrane G protein-coupled receptors; The vasopressin type 2 receptor (V2R) is a G(s)-coupled receptor that controls balance of water and sodium ion by regulating their reabsorption in the renal collecting duct. Mutations of V2R is responsible for nephrogenic diabetes insipidus. Vasopressin (also known as arginine vasopressin or anti-diuretic hormone) is synthesized in the hypothalamus and is released from the posterior pituitary gland. The actions of vasopressin are mediated by the interaction of this hormone with three receptor subtypes: V1aR, V1bR, and V2R. These subtypes are differ in localization, function, and signaling pathways. Activation of V1aR and V1bR stimulate phospholipase C, while activation of V2R stimulates adenylate cyclase. Although vasopressin and oxytocin differ only by two amino acids and stimulate the same cAMP/PKA pathway, they have divergent physiological functions. Vasopressin is involved in regulating blood pressure and the balance of water and sodium ions, whereas oxytocin plays an important role in the uterus during childbirth and in lactation. Pssm-ID: 320510 [Multi-domain] Cd Length: 295 Bit Score: 123.35 E-value: 6.99e-33
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| 7tmA_OT_R | cd15387 | oxytocin receptor, member of the class A family of seven-transmembrane G protein-coupled ... |
36-327 | 3.48e-32 | |||||
oxytocin receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; Oxytocin is a peptide of nine amino acids synthesized in the hypothalamus and is released from the posterior pituitary gland. Oxytocin plays an important role in sexual reproduction of both sexes and is structurally very similar to vasopressin. Although vasopressin and oxytocin differ only by two amino acids and stimulate the same cAMP/PKA pathway, they have divergent physiological functions. Vasopressin is involved in regulating blood pressure and the balance of water and sodium ions, whereas oxytocin plays an important role in the uterus during childbirth and in lactation. Pssm-ID: 320509 [Multi-domain] Cd Length: 297 Bit Score: 121.46 E-value: 3.48e-32
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| 7tmA_GPR150 | cd15198 | G protein-coupled receptor 150, member of the class A family of seven-transmembrane G ... |
70-326 | 1.03e-26 | |||||
G protein-coupled receptor 150, member of the class A family of seven-transmembrane G protein-coupled receptors; GPR150 is an orphan receptor closely related to the oxytocin and vasopressin receptors. Its endogenous ligand is not known. These receptors share a significant amino acid sequence similarity, suggesting that they have a common evolutionary origin. Pssm-ID: 320326 [Multi-domain] Cd Length: 299 Bit Score: 106.82 E-value: 1.03e-26
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| 7tmA_OXR | cd15208 | orexin receptors, member of the class A family of seven-transmembrane G protein-coupled ... |
83-327 | 5.69e-25 | |||||
orexin receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Orexins (OXs, also referred to as hypocretins) are neuropeptide hormones that regulate the sleep-wake cycle and potently influence homeostatic systems regulating appetite and feeding behavior or modulating emotional responses such as anxiety or panic. OXs are synthesized as prepro-orexin (PPO) in the hypothalamus and then proteolytically cleaved into two forms of isoforms: orexin-A (OX-A) and orexin-B (OX-B). OXA is a 33 amino-acid peptide with N-terminal pyroglutamyl residue and two intramolecular disulfide bonds, whereas OXB is a 28 amino-acid linear peptide with no disulfide bonds. OX-A binds orexin receptor 1 (OX1R) with high-affinity, but also binds with somewhat low-affinity to OX2R, and signals primarily to Gq coupling, whereas OX-B shows a strong preference for the orexin receptor 2 (OX2R) and signals through Gq or Gi/o coupling. Thus, activation of OX1R or OX2R will activate phospholipase activity and the phosphatidylinositol and calcium signaling pathways. Additionally, OX2R activation can also lead to inhibition of adenylate cyclase. Pssm-ID: 320336 [Multi-domain] Cd Length: 303 Bit Score: 102.08 E-value: 5.69e-25
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| 7tmA_Opsins_type2_animals | cd14969 | type 2 opsins in animals, member of the class A family of seven-transmembrane G ... |
43-327 | 4.63e-24 | |||||
type 2 opsins in animals, member of the class A family of seven-transmembrane G protein-coupled receptors; This rhodopsin family represents the type 2 opsins found in vertebrates and invertebrates except sponge. Type 2 opsins primarily function as G protein coupled receptors and are responsible for vision as well as for circadian rhythm and pigment regulation. On the contrary, type 1 opsins such as bacteriorhodopsin and proteorhodopsin are found in both prokaryotic and eukaryotic microbes, functioning as light-gated ion channels, proton pumps, sensory receptors and in other unknown functions. Although these two opsin types share seven-transmembrane domain topology and a conserved lysine reside in the seventh helix, type 1 opsins do not activate G-proteins and are not evolutionarily related to type 2. Type 2 opsins can be classified into six distinct subfamilies including the vertebrate opsins/encephalopsins, the G(o) opsins, the G(s) opsins, the invertebrate G(q) opsins, the photoisomerases, and the neuropsins. Pssm-ID: 381741 [Multi-domain] Cd Length: 284 Bit Score: 99.20 E-value: 4.63e-24
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| 7tmA_amine_R-like | cd14967 | amine receptors and similar proteins, member of the class A family of seven-transmembrane G ... |
83-327 | 5.96e-24 | |||||
amine receptors and similar proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; Amine receptors of the class A family of GPCRs include adrenoceptors, 5-HT (serotonin) receptors, muscarinic cholinergic receptors, dopamine receptors, histamine receptors, and trace amine receptors. The receptors of amine subfamily are major therapeutic targets for the treatment of neurological disorders and psychiatric diseases. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320098 [Multi-domain] Cd Length: 259 Bit Score: 98.40 E-value: 5.96e-24
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| 7tmA_NPYR-like | cd15203 | neuropeptide Y receptors and related proteins, member of the class A family of ... |
83-326 | 9.38e-24 | |||||
neuropeptide Y receptors and related proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; NPY is a 36-amino acid peptide neurotransmitter with a C-terminal tyrosine amide residue that is widely distributed in the brain and the autonomic nervous system of many mammalian species. NPY exerts its functions through five, G-protein coupled receptor subtypes including NPY1R, NPY2R, NPY4R, NPY5R, and NPY6R; however, NPY6R is not functional in humans. NYP receptors are also activated by its two other family members, peptide YY (PYY) and pancreatic polypeptide (PP). They typically couple to Gi or Go proteins, which leads to a decrease in adenylate cyclase activity, thereby decreasing intracellular cAMP levels, and are involved in diverse physiological roles including appetite regulation, circadian rhythm, and anxiety. Also included in this subgroup is prolactin-releasing peptide (PrRP) receptor (previously known as GPR10), which is activated by its endogenous ligand PrRP, a neuropeptide possessing C-terminal Arg-Phe-amide motif. There are two active isoforms of PrRP in mammals: one consists of 20 amino acid residues (PrRP-20) and the other consists of 31 amino acid residues (PrRP-31). PrRP receptor shows significant sequence homology to the NPY receptors, and a micromolar level of NPY can bind and completely inhibit the PrRP-evoked intracellular calcium response in PrRP receptor-expressing cells, suggesting that the PrRP receptor shares a common ancestor with the NPY receptors. Pssm-ID: 320331 [Multi-domain] Cd Length: 293 Bit Score: 98.45 E-value: 9.38e-24
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| 7tmA_GPRnna14-like | cd15001 | GPRnna14 and related proteins, member of the class A family of seven-transmembrane G ... |
79-327 | 2.67e-23 | |||||
GPRnna14 and related proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes the orphan G-protein coupled receptor GPRnna14 found in body louse (Pediculus humanus humanus) as well as its closely related proteins of unknown function. These receptors are members of the class A rhodopsin-like G-protein coupled receptors. As an obligatory parasite of humans, the body louse is an important vector for human diseases, including epidemic typhus, relapsing fever, and trench fever. GPRnna14 shares significant sequence similarity with the members of the neurotensin receptor family. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320132 [Multi-domain] Cd Length: 266 Bit Score: 96.96 E-value: 2.67e-23
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| 7tmA_purinoceptor-like | cd14982 | purinoceptor and its related proteins, member of the class A family of seven-transmembrane G ... |
69-327 | 4.96e-23 | |||||
purinoceptor and its related proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; Members of this subfamily include lysophosphatidic acid receptor, P2 purinoceptor, protease-activated receptor, platelet-activating factor receptor, Epstein-Barr virus induced gene 2, proton-sensing G protein-coupled receptors, GPR35, and GPR55, among others. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 341318 [Multi-domain] Cd Length: 283 Bit Score: 96.57 E-value: 4.96e-23
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| 7tmA_Galanin_R-like | cd14971 | galanin receptor and related proteins, member of the class A family of seven-transmembrane G ... |
78-327 | 6.10e-22 | |||||
galanin receptor and related proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This subfamily includes G-protein coupled galanin receptors, kisspeptin receptor and allatostatin-A receptor (AstA-R) in insects. These receptors, which are members of the class A of seven transmembrane GPCRs, share a high degree of sequence homology among themselves. The galanin receptors bind galanin, a neuropeptide that is widely expressed in the brain, peripheral tissues, and endocrine glands. Galanin is implicated in numerous neurological and psychiatric diseases including Alzheimer's disease, eating disorders, and epilepsy, among many others. KiSS1-derived peptide receptor (also known as GPR54 or kisspeptin receptor) binds the peptide hormone kisspeptin (metastin), which encoded by the metastasis suppressor gene (KISS1) expressed in various endocrine and reproductive tissues. AstA-R is a G-protein coupled receptor that binds allatostatin A. Three distinct types of allatostatin have been identified in the insects and crustaceans: AstA, AstB, and AstC. They both inhibit the biosynthesis of juvenile hormone and exert an inhibitory influence on food intake. Therefore, allatostatins are considered as potential targets for insect control. Pssm-ID: 320102 [Multi-domain] Cd Length: 281 Bit Score: 93.30 E-value: 6.10e-22
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| 7tmA_Anaphylatoxin_R-like | cd14974 | anaphylatoxin receptors and related G protein-coupled chemokine receptors, member of the class ... |
82-326 | 9.55e-22 | |||||
anaphylatoxin receptors and related G protein-coupled chemokine receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; This subfamily of G-protein coupled receptors includes anaphylatoxin receptors, formyl peptide receptors (FPR), prostaglandin D2 receptor 2, GPR1, and related chemokine receptors. The anaphylatoxin receptors are a group of G-protein coupled receptors that bind anaphylatoxins. The members of this group include C3a and C5a receptors. The formyl peptide receptors (FPRs) are chemoattractant GPCRs that involved in mediating immune responses to infection. They are expressed mainly on polymorphonuclear and mononuclear phagocytes and bind N-formyl-methionyl peptides (FMLP), which are derived from the mitochondrial proteins of ruptured host cells or invading pathogens. Chemokine receptor-like 1 (also known as chemerin receptor 23) is a GPCR for the chemoattractant adipokine chemerin, also known as retinoic acid receptor responder protein 2 (RARRES2), and for the omega-3 fatty acid derived molecule resolvin E1. Interaction with chemerin induces activation of the MAPK and PI3K signaling pathways leading to downstream functional effects, such as a decrease in immune responses, stimulation of adipogenesis, and angiogenesis. On the other hand, resolvin E1 negatively regulates the cytokine production in macrophages by reducing the activation of MAPK1/3 and NF-kB pathways. Prostaglandin D2 receptor, also known as CRTH2, is a chemoattractant G-protein coupled receptor expressed on T helper type 2 cells that binds prostaglandin D2 (PGD2). PGD2 functions as a mast cell-derived mediator to trigger asthmatic responses and also causes vasodilation. PGD2 exerts its inflammatory effects by binding to two G-protein coupled receptors, the D-type prostanoid receptor (DP) and PD2R2 (CRTH2). PD2R2 couples to the G protein G(i/o) type which leads to a reduction in intracellular cAMP levels and an increase in intracellular calcium. GPR1 is an orphan receptor that can be activated by the leukocyte chemoattractant chemerin, thereby suggesting that some of the anti-inflammatory actions of chemerin may be mediated through GPR1. Pssm-ID: 320105 [Multi-domain] Cd Length: 274 Bit Score: 92.75 E-value: 9.55e-22
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| 7tmA_Bombesin_R-like | cd15927 | bombesin receptor subfamily, member of the class A family of seven-transmembrane G ... |
83-321 | 1.22e-21 | |||||
bombesin receptor subfamily, member of the class A family of seven-transmembrane G protein-coupled receptors; This bombesin subfamily of G-protein coupled receptors consists of neuromedin B receptor (NMBR), gastrin-releasing peptide receptor (GRPR), and bombesin receptor subtype 3 (BRS-3). Bombesin is a tetradecapeptide, originally isolated from frog skin. Mammalian bombesin-related peptides are widely distributed in the gastrointestinal and central nervous systems. The bombesin family receptors couple mainly to the G proteins of G(q/11) family. NMBR functions as the receptor for the neuropeptide neuromedin B, a potent mitogen and growth factor for normal and cancerous lung and for gastrointestinal epithelial tissues. Gastrin-releasing peptide is an endogenous ligand for GRPR and shares high sequence homology with NMB in the C-terminal region. Both NMB and GRP possess bombesin-like biochemical properties. BRS-3 is classified as an orphan receptor and suggested to play a role in sperm cell division and maturation. BRS-3 interacts with known naturally-occurring bombesin-related peptides with low affinity; however, no endogenous high-affinity ligand to the receptor has been identified. The bombesin receptor family belongs to the seven transmembrane rhodopsin-like G-protein coupled receptors (class A GPCRs), which perceive extracellular signals and transduce them to guanine nucleotide-binding (G) proteins. Pssm-ID: 320593 [Multi-domain] Cd Length: 294 Bit Score: 92.72 E-value: 1.22e-21
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| 7tmA_NPFFR | cd15207 | neuropeptide FF receptors, member of the class A family of seven-transmembrane G ... |
83-327 | 2.23e-21 | |||||
neuropeptide FF receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Neuropeptide FF (NPFF) is a mammalian octapeptide that belongs to a family of neuropeptides containing an RF-amide motif at their C-terminus that have been implicated in a wide range of physiological functions in the brain including pain sensitivity, insulin release, food intake, memory, blood pressure, and opioid-induced tolerance and hyperalgesia. The effects of these peptides are mediated through neuropeptide FF1 and FF2 receptors (NPFF1-R and NPFF2-R) which are predominantly expressed in the brain. NPFF induces pro-nociceptive effects, mainly through the NPFF1-R, and anti-nociceptive effects, mainly through the NPFF2-R. NPFF has been shown to inhibit adenylate cyclase via the Gi protein coupled to NPFF1-R. Pssm-ID: 320335 [Multi-domain] Cd Length: 291 Bit Score: 91.91 E-value: 2.23e-21
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| 7tmA_Gal1_R | cd15098 | galanin receptor subtype 1, member of the class A family of seven-transmembrane G ... |
66-327 | 9.80e-21 | |||||
galanin receptor subtype 1, member of the class A family of seven-transmembrane G protein-coupled receptors; The G protein-coupled galanin receptors bind galanin, a neuropeptide that is widely expressed in the brain, peripheral tissues, and endocrine glands. Three receptors subtypes have been so far identified: GAL1, GAL2, and GAL3. The specific functions of each subtype remains mostly unknown, although galanin is thought to be involved in a variety of neuronal functions such as hormone release and food intake. Galanin is implicated in numerous neurological and psychiatric diseases including Alzheimer's disease, depression, eating disorders, epilepsy and stroke, among many others. Pssm-ID: 320226 [Multi-domain] Cd Length: 282 Bit Score: 90.17 E-value: 9.80e-21
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| 7tmA_TACR_family | cd14992 | tachykinin receptor and closely related proteins, member of the class A family of ... |
78-323 | 2.82e-20 | |||||
tachykinin receptor and closely related proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This subfamily includes G-protein coupled receptors for a variety of neuropeptides of the tachykinin (TK) family as well as closely related receptors. The tachykinins are widely distributed throughout the mammalian central and peripheral nervous systems and act as excitatory transmitters on neurons and cells in the gastrointestinal tract. The TKs are characterized by a common five-amino acid C-terminal sequence, Phe-X-Gly-Leu-Met-NH2, where X is a hydrophobic residue. The three major mammalian tachykinins are substance P (SP), neurokinin A (NKA), and neurokinin B (NKB). The physiological actions of tachykinins are mediated through three types of receptors: neurokinin receptor type 1 (NK1R), NK2R, and NK3R. SP is a high-affinity endogenous ligand for NK1R, which interacts with the Gq protein and activates phospholipase C, leading to elevation of intracellular calcium. NK2R is a high-affinity receptor for NKA, the tachykinin neuropeptide substance K. SP and NKA are found in the enteric nervous system and mediate in the regulation of gastrointestinal motility, secretion, vascular permeability, and pain perception. NK3R is activated by its high-affinity ligand, NKB, which is primarily involved in the central nervous system and plays a critical role in the regulation of gonadotropin hormone release and the onset of puberty. Pssm-ID: 320123 [Multi-domain] Cd Length: 291 Bit Score: 89.03 E-value: 2.82e-20
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| 7tmA_TAARs | cd15055 | trace amine-associated receptors, member of the class A family of seven-transmembrane G ... |
78-326 | 1.08e-19 | |||||
trace amine-associated receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; The trace amine-associated receptors (TAARs) are a distinct subfamily within the class A G protein-coupled receptor family. Trace amines are endogenous amines of unknown function that have strong structural and metabolic similarity to classical monoamine neurotransmitters (serotonin, noradrenaline, adrenaline, dopamine, and histamine), which play critical roles in human and animal physiological activities such as cognition, consciousness, mood, motivation, perception, and autonomic responses. However, trace amines are found in the mammalian brain at very low concentrations compared to classical monoamines. Trace amines, including p-tyramine, beta-phenylethylamine, and tryptamine, are also thought to act as chemical messengers to exert their biological effects in vertebrates. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320183 [Multi-domain] Cd Length: 285 Bit Score: 87.22 E-value: 1.08e-19
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| 7tmA_Gal2_Gal3_R | cd15097 | galanin receptor subtypes 2 and 3, member of the class A family of seven-transmembrane G ... |
78-327 | 1.57e-19 | |||||
galanin receptor subtypes 2 and 3, member of the class A family of seven-transmembrane G protein-coupled receptors; The G protein-coupled galanin receptors bind galanin, a neuropeptide that is widely expressed in the brain, peripheral tissues, and endocrine glands. Three receptors subtypes have been so far identified: GAL1, GAL2, and GAL3. The specific functions of each subtype remains mostly unknown, although galanin is thought to be involved in a variety of neuronal functions such as hormone release and food intake. Galanin is implicated in numerous neurological and psychiatric diseases including Alzheimer's disease, depression, eating disorders, epilepsy and stroke, among many others. Pssm-ID: 320225 [Multi-domain] Cd Length: 279 Bit Score: 86.80 E-value: 1.57e-19
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| 7tmA_PR4-like | cd15392 | neuropeptide Y receptor-like found in insect and related proteins, member of the class A ... |
76-325 | 5.48e-19 | |||||
neuropeptide Y receptor-like found in insect and related proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This subgroup includes a novel G protein-coupled receptor (also known as PR4 receptor) from Drosophila melanogaster, which can be activated by the members of the neuropeptide Y (NPY) family, including NPY, peptide YY (PYY) and pancreatic polypeptide (PP), when expressed in Xenopus oocytes. These homologous peptides of 36-amino acids in length contain a hairpin-like structural motif, which referred to as the pancreatic polypeptide fold, and function as gastrointestinal hormones and neurotransmitters. The PR4 receptor also shares strong sequence homology to the mammalian tachykinin receptors (NK1R, NK2R, and NK3R), whose endogenous ligands are substance P (SP), neurokinin A (NKA), and neurokinin B (NKB), respectively. The tachykinins function as excitatory transmitters on neurons and cells in the gastrointestinal tract. Pssm-ID: 320514 [Multi-domain] Cd Length: 287 Bit Score: 85.49 E-value: 5.48e-19
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| 7tmA_QRFPR | cd15205 | pyroglutamylated RFamide peptide receptor, member of the class A family of seven-transmembrane ... |
83-325 | 5.79e-19 | |||||
pyroglutamylated RFamide peptide receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; 26RFa, also known as QRFP (Pyroglutamylated RFamide peptide), is a 26-amino acid residue peptide that belongs to a family of neuropeptides containing an Arg-Phe-NH2 (RFamide) motif at its C-terminus. 26Rfa/QRFP exerts similar orexigenic activity including the regulation of feeding behavior in mammals. It is the ligand for G-protein coupled receptor 103 (GPR103), which is predominantly expressed in paraventricular (PVN) and ventromedial (VMH) nuclei of the hypothalamus. GPR103 shares significant protein sequence homology with orexin receptors (OX1R and OX2R), which have recently shown to produce a neuroprotective effect in Alzheimer's disease by forming a functional heterodimer with GPR103. Pssm-ID: 320333 [Multi-domain] Cd Length: 298 Bit Score: 85.60 E-value: 5.79e-19
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| 7tmA_prokineticin-R | cd15204 | prokineticin receptors, member of the class A family of seven-transmembrane G protein-coupled ... |
78-308 | 1.34e-18 | |||||
prokineticin receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Prokineticins 1 (PROK1) and 2 (PROK2), also known as endocrine gland vascular endothelial factor and Bombina varigata 8, respectively, are multifunctional chemokine-like peptides that are highly conserved across species. Prokineticins can bind with similar affinities to two closely homologous 7-transmembrane G protein coupled receptors, PROKR1 and PROKR2, which are phylogenetically related to the tachykinin receptors. Prokineticins and their GPCRs are widely distributed in human tissues and are involved in numerous physiological roles, including gastrointestinal motility, generation of circadian rhythms, neuron migration and survival, pain sensation, angiogenesis, inflammation, and reproduction. Moreover, different point mutations in genes encoding PROK2 or its receptor (PROKR2) can lead to Kallmann syndrome, a disease characterized by delayed or absent puberty and impaired olfactory function. Pssm-ID: 320332 [Multi-domain] Cd Length: 288 Bit Score: 84.25 E-value: 1.34e-18
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| 7tmA_TACR | cd15390 | neurokinin receptors (or tachykinin receptors), member of the class A family of ... |
80-323 | 1.80e-18 | |||||
neurokinin receptors (or tachykinin receptors), member of the class A family of seven-transmembrane G protein-coupled receptors; This group represents G-protein coupled receptors for a variety of neuropeptides of the tachykinin (TK) family. The tachykinins are widely distributed throughout the mammalian central and peripheral nervous systems and act as excitatory transmitters on neurons and cells in the gastrointestinal tract. The TKs are characterized by a common five-amino acid C-terminal sequence, Phe-X-Gly-Leu-Met-NH2, where X is a hydrophobic residue. The three major mammalian tachykinins are substance P (SP), neurokinin A (NKA), and neurokinin B (NKB). The physiological actions of tachykinins are mediated through three types of receptors: neurokinin receptor type 1 (NK1R), NK2R, and NK3R. SP is a high-affinity endogenous ligand for NK1R, which interacts with the Gq protein and activates phospholipase C, leading to elevation of intracellular calcium. NK2R is a high-affinity receptor for NKA, the tachykinin neuropeptide substance K. SP and NKA are found in the enteric nervous system and mediate in the regulation of gastrointestinal motility, secretion, vascular permeability, and pain perception. NK3R is activated by its high-affinity ligand, NKB, which is primarily involved in the central nervous system and plays a critical role in the regulation of gonadotropin hormone release and the onset of puberty. Pssm-ID: 320512 [Multi-domain] Cd Length: 289 Bit Score: 83.88 E-value: 1.80e-18
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| 7tmA_C5aR | cd15114 | complement component 5a anaphylatoxin chemotactic receptors, member of the class A family of ... |
82-326 | 2.43e-18 | |||||
complement component 5a anaphylatoxin chemotactic receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; The anaphylatoxin receptors are a group of G-protein coupled receptors which bind anaphylatoxins; members of this group include C3a receptors and C5a receptors. Anaphylatoxins are also known as complement peptides (C3a, C4a and C5a) that are produced from the activation of the complement system cascade. These complement anaphylatoxins can trigger degranulation of endothelial cells, mast cells, or phagocytes, which induce a local inflammatory response and stimulate smooth muscle cell contraction, histamine release, and increased vascular permeability. They are potent mediators involved in chemotaxis, inflammation, and generation of cytotoxic oxygen-derived free radicals. In humans, a single receptor for C3a (C3AR1) and two receptors for C5a (C5AR1 and C5AR2, also known as C5L2 or GPR77) have been identified, but there is no known receptor for C4a. Pssm-ID: 320242 [Multi-domain] Cd Length: 274 Bit Score: 83.22 E-value: 2.43e-18
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| 7tmA_Opioid_R-like | cd14970 | opioid receptors and related proteins, member of the class A family of seven-transmembrane G ... |
72-327 | 3.12e-18 | |||||
opioid receptors and related proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes opioid receptors, somatostatin receptors, melanin-concentrating hormone receptors (MCHRs), and neuropeptides B/W receptors. Together they constitute the opioid receptor-like family, members of the class A G-protein coupled receptors. Opioid receptors are coupled to inhibitory G proteins of the G(i/o) family and are involved in regulating a variety of physiological functions such as pain, addiction, mood, stress, epileptic seizure, and obesity, among many others. G protein-coupled somatostatin receptors (SSTRs), which display strong sequence similarity with opioid receptors, binds somatostatin (somatotropin release inhibiting factor), a polypeptide hormone that regulates a wide variety of physiological functions such as neurotransmission, cell proliferation, contractility of smooth muscle cells, and endocrine signaling as well as inhibition of the release of many secondary hormones. MCHR binds melanin concentrating hormone and is presumably involved in the neuronal regulation of food intake. Despite strong homology with somatostatin receptors, MCHR does not appear to bind somatostatin. Neuropeptides B/W receptors are primarily expressed in the CNS and stimulate the cortisol secretion by activating the adenylate cyclase- and the phospholipase C-dependent signaling pathways. Pssm-ID: 320101 [Multi-domain] Cd Length: 282 Bit Score: 83.11 E-value: 3.12e-18
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| 7tmA_BRS-3 | cd15123 | bombesin receptor subtype 3, member of the class A family of seven-transmembrane G ... |
78-327 | 5.42e-18 | |||||
bombesin receptor subtype 3, member of the class A family of seven-transmembrane G protein-coupled receptors; BRS-3 is classified as an orphan receptor and belongs to the bombesin subfamily of G-protein coupled receptors, whose members also include neuromedin B receptor (NMBR) and gastrin-releasing peptide receptor (GRPR). Bombesin is a tetradecapeptide, originally isolated from frog skin. Mammalian bombesin-related peptides are widely distributed in the gastrointestinal and central nervous systems. The bombesin family receptors couple primarily to the G proteins of G(q/11) family. BRS-3 interacts with known naturally-occurring bombesin-related peptides with low affinity; however, no endogenous high-affinity ligand to the receptor has been identified. BRS-3 is suggested to play a role in sperm cell division and maturation. Pssm-ID: 320251 [Multi-domain] Cd Length: 294 Bit Score: 82.66 E-value: 5.42e-18
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| 7tmA_Angiotensin_R-like | cd14985 | angiotesin receptor family and its related G protein-coupled receptors, member of the class A ... |
107-326 | 6.53e-18 | |||||
angiotesin receptor family and its related G protein-coupled receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes the angiotensin receptors, the bradykinin receptors, apelin receptor as well as putative G-protein coupled receptors (GPR15 and GPR25). Angiotensin II (Ang II), the main effector in the renin-angiotensin system, plays a crucial role in the regulation of cardiovascular homeostasis through its type 1 (AT1) and type 2 (AT2) receptors. Ang II contributes to cardiovascular diseases such as hypertension and atherosclerosis via AT1R activation. Ang II increases blood pressure through Gq-mediated activation of phospholipase C, resulting in phosphoinositide (PI) hydrolysis and increased intracellular calcium levels. Through the AT2 receptor, Ang II counteracts the vasoconstrictor action of AT1R and thereby induces vasodilation, sodium excretion, and reduction of blood pressure. Bradykinins (BK) are pro-inflammatory peptides that mediate various vascular and pain responses to tissue injury through its B1 and B2 receptors. Apelin (APJ) receptor binds the endogenous peptide ligands, apelin and Toddler/Elabela. APJ is an adipocyte-derived hormone that is ubiquitously expressed throughout the human body, and Toddler/Elabela is a short secretory peptide that is required for normal cardiac development in zebrafish. Activation of APJ receptor plays key roles in diverse physiological processes including vasoconstriction and vasodilation, cardiac muscle contractility, angiogenesis, and regulation of water balance and food intake. Orphan receptors, GPR15 and GPR25, share strong sequence homology to the angiotensin II type AT1 and AT2 receptors. Pssm-ID: 341320 [Multi-domain] Cd Length: 284 Bit Score: 82.43 E-value: 6.53e-18
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| 7tmA_5-HT7 | cd15329 | serotonin receptor subtype 7, member of the class A family of seven-transmembrane G ... |
71-327 | 1.82e-17 | |||||
serotonin receptor subtype 7, member of the class A family of seven-transmembrane G protein-coupled receptors; The 5-HT7 receptor, one of 14 mammalian serotonin receptors, is a member of the class A of GPCRs and is activated by the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). 5-HT7 receptor mainly couples to Gs protein, which positively stimulates adenylate cyclase, leading to increased intracellular cAMP formation and calcium influx. 5-HT7 receptor is expressed in various human tissues, mainly in the brain, the lower gastrointestinal tract and in vital blood vessels including the coronary artery. In the CNS, serotonin is involved in the regulation of appetite, mood, sleep, cognition, learning and memory, as well as implicated in neurologic disorders such as migraine, schizophrenia, and depression. Pssm-ID: 320452 [Multi-domain] Cd Length: 260 Bit Score: 80.39 E-value: 1.82e-17
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| 7tmA_Apelin_R | cd15190 | apelin receptor, member of the class A family of seven-transmembrane G protein-coupled ... |
40-328 | 2.19e-17 | |||||
apelin receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; Apelin (APJ) receptor is a G protein-coupled receptor that binds the endogenous peptide ligands, apelin and Toddler/Elabela. APJ is an adipocyte-derived hormone that is ubiquitously expressed throughout the human body and Toddler/Elabela is a short secretory peptide that is required for normal cardiac development in zebrafish. Activation of APJ receptor plays key roles in diverse physiological processes including vasoconstriction and vasodilation, cardiac muscle contractility, angiogenesis, and regulation of water balance and food intake. Pssm-ID: 341340 [Multi-domain] Cd Length: 304 Bit Score: 80.96 E-value: 2.19e-17
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| 7tmA_NMBR | cd15125 | neuromedin B receptor, member of the class A family of seven-transmembrane G protein-coupled ... |
78-321 | 4.76e-17 | |||||
neuromedin B receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; The neuromedin B receptor (NMBR), also known as BB1, is a G-protein coupled receptor whose endogenous ligand is the neuropeptide neuromedin B. Neuromedin B is a potent mitogen and growth factor for normal and cancerous lung and for gastrointestinal epithelial tissues. NMBR is widely distributed in the CNS, with especially high levels in olfactory nucleus and thalamic regions. The receptor couples primarily to a pertussis-toxin-insensitive G protein of the Gq/11 family, which leads to the activation of phospholipase C. NMBR belongs to the bombesin subfamily of G-protein coupled receptors, whose members also include gastrin-releasing peptide receptor (GRPR) and bombesin receptor subtype 3 (BRS-3). Bombesin is a tetradecapeptide, originally isolated from frog skin. Pssm-ID: 320253 [Multi-domain] Cd Length: 292 Bit Score: 79.99 E-value: 4.76e-17
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| 7tmA_ETH-R | cd14997 | ecdysis-triggering hormone receptors, member of the class A family of seven-transmembrane G ... |
74-327 | 7.28e-17 | |||||
ecdysis-triggering hormone receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; This subgroup represents the ecdysis-triggering hormone receptors found in insects, which are members of the class A family of seven-transmembrane G-protein coupled receptors. Ecdysis-triggering hormones are vital regulatory signals that govern the stereotypic physiological sequence leading to cuticle shedding in insects. Thus, the ETH signaling system has been a target for the design of more sophisticated insect-selective pest control strategies. Two subtypes of ecdysis-triggering hormone receptor were identified in Drosophila melanogaster. Blood-borne ecdysis-triggering hormone (ETH) activates the behavioral sequence through direct actions on the central nervous system. In insects, ecdysis is thought to be controlled by the interaction between peptide hormones; in particular between ecdysis-triggering hormone (ETH) from the periphery and eclosion hormone (EH) and crustacean cardioactive peptide (CCAP) from the central nervous system. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320128 [Multi-domain] Cd Length: 294 Bit Score: 79.26 E-value: 7.28e-17
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| 7tmA_5-HT1_5_7 | cd15064 | serotonin receptor subtypes 1, 5 and 7, member of the class A family of seven-transmembrane G ... |
79-327 | 7.52e-17 | |||||
serotonin receptor subtypes 1, 5 and 7, member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes serotonin receptor subtypes 1, 5, and 7 that are activated by the neurotransmitter serotonin. The 5-HT1 and 5-HT5 receptors mediate inhibitory neurotransmission by coupling to G proteins of the G(i/o) family. The 5-HT1 receptor subfamily includes 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F. There is no 5-HT1C receptor subtype, as it has been reclassified as 5-HT2C receptor. The 5-HT5A and 5-HT5B receptors have been cloned from rat and mouse, but only the 5-HT5A isoform has been identified in human because of the presence of premature stop codons in the human 5-HT5B gene, which prevents a functional receptor from being expressed. The 5-HT7 receptor is coupled to Gs, which positively stimulates adenylate cyclase activity, leading to increased intracellular cAMP formation and calcium influx. In the CNS, serotonin is involved in the regulation of appetite, mood, sleep, cognition, learning and memory, as well as implicated in neurologic disorders such as migraine, schizophrenia, and depression. Pssm-ID: 320192 [Multi-domain] Cd Length: 258 Bit Score: 78.91 E-value: 7.52e-17
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| 7tmA_TACR-like | cd15202 | tachykinin receptors and related receptors, member of the class A family of ... |
78-326 | 9.48e-17 | |||||
tachykinin receptors and related receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes the neurokinin/tachykinin receptors and its closely related receptors such as orphan GPR83 and leucokinin-like peptide receptor. The tachykinins are widely distributed throughout the mammalian central and peripheral nervous systems and act as excitatory transmitters on neurons and cells in the gastrointestinal tract. The TKs are characterized by a common five-amino acid C-terminal sequence, Phe-X-Gly-Leu-Met-NH2, where X is a hydrophobic residue. The three major mammalian tachykinins are substance P (SP), neurokinin A (NKA), and neurokinin B (NKB). The physiological actions of tachykinins are mediated through three types of receptors: neurokinin receptor type 1 (NK1R), NK2R, and NK3R. SP is a high-affinity endogenous ligand for NK1R, which interacts with the Gq protein and activates phospholipase C, leading to elevation of intracellular calcium. NK2R is a high-affinity receptor for NKA, the tachykinin neuropeptide substance K. SP and NKA are found in the enteric nervous system and mediate in the regulation of gastrointestinal motility, secretion, vascular permeability, and pain perception. NK3R is activated by its high-affinity ligand, NKB, which is primarily involved in the central nervous system and plays a critical role in the regulation of gonadotropin hormone release and the onset of puberty. Pssm-ID: 320330 [Multi-domain] Cd Length: 288 Bit Score: 79.09 E-value: 9.48e-17
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| 7tmA_TAAR1 | cd15314 | trace amine-associated receptor 1 and similar receptors, member of the class A family of ... |
83-326 | 2.19e-16 | |||||
trace amine-associated receptor 1 and similar receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; The trace amine-associated receptor 1 (TAAR1) is one of the 15 identified trace amine-associated receptor subtypes, which form a distinct subfamily within the class A G protein-coupled receptor family. Trace amines are endogenous amines of unknown function that have strong structural and metabolic similarity to classical monoamine neurotransmitters (serotonin, noradrenaline, adrenaline, dopamine, and histamine), which play critical roles in human and animal physiological activities such as cognition, consciousness, mood, motivation, perception, and autonomic responses. However, trace amines are found in the mammalian brain at very low concentrations compared to classical monoamines. TAAR1 is coupled to the Gs protein, which leads to activation of adenylate cyclase, and is thought to play functional role in the regulation of brain monoamines. TAAR1 is also shown to be activated by psychoactive compounds such as Ecstasy (MDMA), amphetamine and LSD. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320438 [Multi-domain] Cd Length: 282 Bit Score: 78.05 E-value: 2.19e-16
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| 7tmA_CCK_R | cd15206 | cholecystokinin receptors, member of the class A family of seven-transmembrane G ... |
80-323 | 2.51e-16 | |||||
cholecystokinin receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Cholecystokinin receptors (CCK-AR and CCK-BR) are a group of G-protein coupled receptors which bind the peptide hormones cholecystokinin (CCK) or gastrin. CCK, which facilitates digestion in the small intestine, and gastrin, a major regulator of gastric acid secretion, are highly similar peptides. Like gastrin, CCK is a naturally-occurring linear peptide that is synthesized as a preprohormone, then proteolytically cleaved to form a family of peptides with the common C-terminal sequence (Gly-Trp-Met-Asp-Phe-NH2), which is required for full biological activity. CCK-AR (type A, alimentary; also known as CCK1R) is found abundantly on pancreatic acinar cells and binds only sulfated CCK-peptides with very high affinity, whereas CCK-BR (type B, brain; also known as CCK2R), the predominant form in the brain and stomach, binds CCK or gastrin and discriminates poorly between sulfated and non-sulfated peptides. CCK is implicated in regulation of digestion, appetite control, and body weight, and is involved in neurogenesis via CCK-AR. There is some evidence to support that CCK and gastrin, via their receptors, are involved in promoting cancer development and progression, acting as growth and invasion factors. Pssm-ID: 320334 [Multi-domain] Cd Length: 269 Bit Score: 77.43 E-value: 2.51e-16
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| 7tmA_C3aR | cd15115 | complement component 3a anaphylatoxin chemotactic receptors, member of the class A family of ... |
106-323 | 3.90e-16 | |||||
complement component 3a anaphylatoxin chemotactic receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; The anaphylatoxin receptors are a group of G-protein coupled receptors which bind anaphylatoxins; members of this group include C3a receptors and C5a receptors. Anaphylatoxins are also known as complement peptides (C3a, C4a and C5a) that are produced from the activation of the complement system cascade. These complement anaphylatoxins can trigger degranulation of endothelial cells, mast cells, or phagocytes, which induce a local inflammatory response and stimulate smooth muscle cell contraction, histamine release, and increased vascular permeability. They are potent mediators involved in chemotaxis, inflammation, and generation of cytotoxic oxygen-derived free radicals. In humans, a single receptor for C3a (C3AR1) and two receptors for C5a (C5AR1 and C5AR2, also known as C5L2 or GPR77) have been identified, but there is no known receptor for C4a. Pssm-ID: 320243 [Multi-domain] Cd Length: 265 Bit Score: 76.73 E-value: 3.90e-16
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| 7tmA_TAAR5-like | cd15317 | trace amine-associated receptor 5 and similar receptors, member of the class A family of ... |
78-326 | 4.26e-16 | |||||
trace amine-associated receptor 5 and similar receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Included in this group are mammalian TAAR5, TAAR6, TAAR8, TAAR9, and similar proteins. They are among the 15 identified trace amine-associated receptors (TAARs), a distinct subfamily within the class A G protein-coupled receptors. Trace amines are endogenous amines of unknown function that have strong structural and metabolic similarity to classical monoamine neurotransmitters (serotonin, noradrenaline, adrenaline, dopamine, and histamine), which play critical roles in human and animal physiological activities such as cognition, consciousness, mood, motivation, perception, and autonomic responses. However, trace amines are found in the mammalian brain at very low concentrations compared to classical monoamines. Trace amines, including p-tyramine, beta-phenylethylamine, and tryptamine, are also thought to act as chemical messengers to exert their biological effects in vertebrates. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320440 [Multi-domain] Cd Length: 290 Bit Score: 77.10 E-value: 4.26e-16
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| 7tmA_Dop1R2-like | cd15067 | dopamine 1-like receptor 2 from Drosophila melanogaster and similar proteins, member of the ... |
83-327 | 7.10e-16 | |||||
dopamine 1-like receptor 2 from Drosophila melanogaster and similar proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; G protein-coupled dopamine 1-like receptor 2 is expressed in Drosophila heads and it shows significant sequence similarity with vertebrate and invertebrate dopamine receptors. Although the Drosophila Dop1R2 receptor does not cluster into the D1-like structural group, it does show pharmacological properties similar to D1-like receptors. As shown in vertebrate D1-like receptors, agonist stimulation of Dop1R2 activates adenylyl cyclase to increase cAMP levels and also generates a calcium signal through stimulation of phospholipase C. Pssm-ID: 320195 [Multi-domain] Cd Length: 262 Bit Score: 76.24 E-value: 7.10e-16
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| 7tmA_GRPR | cd15124 | gastrin-releasing peptide receptor, member of the class A family of seven-transmembrane G ... |
78-321 | 9.07e-16 | |||||
gastrin-releasing peptide receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; The gastrin-releasing peptide receptor (GRPR) is a G-protein coupled receptor whose endogenous ligand is gastrin releasing peptide. GRP shares high sequence homology with the neuropeptide neuromedin B in the C-terminal region. This receptor is high glycosylated and couples to a pertussis-toxin-insensitive G protein of the family of Gq/11, which leads to the activation of phospholipase C. Gastrin-releasing peptide (GRP) is a potent mitogen for neoplastic tissues and involved in regulating multiple functions of the gastrointestinal and central nervous systems. These include the release of gastrointestinal hormones, the contraction of smooth muscle cells, and the proliferation of epithelial cells. GRPR belongs to the bombesin subfamily of G-protein coupled receptors, whose members also include neuromedin B receptor (NMBR) and bombesin receptor subtype 3 (BRS-3). Bombesin is a tetradecapeptide, originally isolated from frog skin. Pssm-ID: 320252 [Multi-domain] Cd Length: 293 Bit Score: 76.48 E-value: 9.07e-16
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| 7tmA_UII-R | cd14999 | urotensin-II receptor, member of the class A family of seven-transmembrane G protein-coupled ... |
69-323 | 3.15e-15 | |||||
urotensin-II receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; The urotensin-II receptor (UII-R, also known as the hypocretin receptor) is a member of the class A rhodopsin-like G-protein coupled receptors, which binds the peptide hormone urotensin-II. Urotensin II (UII) is a vasoactive somatostatin-like or cortistatin-like peptide hormone. However, despite the apparent structural similarity to these peptide hormones, they are not homologous to UII. Urotensin II was first identified in fish spinal cord, but later found in humans and other mammals. In fish, UII is secreted at the back part of the spinal cord, in a neurosecretory centre called uroneurapophysa, and is involved in the regulation of the renal and cardiovascular systems. In mammals, urotensin II is the most potent mammalian vasoconstrictor identified to date and causes contraction of arterial blood vessels, including the thoracic aorta. The urotensin II receptor is a rhodopsin-like G-protein coupled receptor, which binds urotensin-II. The receptor was previously known as GPR14, or sensory epithelial neuropeptide-like receptor (SENR). The UII receptor is expressed in the CNS (cerebellum and spinal cord), skeletal muscle, pancreas, heart, endothelium and vascular smooth muscle. It is involved in the pathophysiological control of cardiovascular function and may also influence CNS and endocrine functions. Binding of urotensin II to the receptor leads to activation of phospholipase C, through coupling to G(q/11) family proteins. The resulting increase in intracellular calcium may cause the contraction of vascular smooth muscle. Pssm-ID: 320130 [Multi-domain] Cd Length: 282 Bit Score: 74.79 E-value: 3.15e-15
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| 7tmA_GPR83 | cd15389 | G protein-coupled receptor 83, member of the class A family of seven-transmembrane G ... |
78-323 | 7.35e-15 | |||||
G protein-coupled receptor 83, member of the class A family of seven-transmembrane G protein-coupled receptors; GPR83, also known as GPR72, is widely expressed in the brain, including hypothalamic nuclei which is involved in regulating energy balance and food intake. The hypothalamic expression of GPR83 is tightly regulated in response to nutrient availability and is decreased in obese mice. A recent study suggests that GPR83 has a critical role in the regulation of systemic energy metabolism via ghrelin-dependent and ghrelin-independent mechanisms. GPR83 shares a significant amino acid sequence identity with the tachykinin receptors, however its endogenous ligand is unknown. Pssm-ID: 320511 [Multi-domain] Cd Length: 285 Bit Score: 73.53 E-value: 7.35e-15
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| 7tmA_LTB4R | cd14975 | leukotriene B4 receptors, member of the class A family of seven-transmembrane G ... |
69-288 | 1.29e-14 | |||||
leukotriene B4 receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Leukotriene B4 (LTB4), a metabolite of arachidonic acid, is a powerful chemotactic activator for granulocytes and macrophages. Two receptors for LTB4 have been identified: a high-affinity receptor (LTB4R1 or BLT1) and a low-affinity receptor (TB4R2 or BLT2). Both BLT1 and BLT2 receptors belong to the rhodopsin-like G-protein coupled receptor superfamily and primarily couple to G(i) proteins, which lead to chemotaxis, calcium mobilization, and inhibition of adenylate cyclase. In some cells, they can also couple to the G(q)-like protein, G16, and activate phospholipase C. LTB4 is involved in mediating inflammatory processes, immune responses, and host defense against infection. Studies have shown that LTB4 stimulates leukocyte extravasation, neutrophil degranulation, lysozyme release, and reactive oxygen species generation. Pssm-ID: 320106 [Multi-domain] Cd Length: 278 Bit Score: 72.90 E-value: 1.29e-14
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| 7tmA_Chemokine_R | cd14984 | classical and atypical chemokine receptors, member of the class A family of ... |
80-325 | 1.36e-14 | |||||
classical and atypical chemokine receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Chemokines are principal regulators for leukocyte trafficking, recruitment, and activation. Chemokine family membership is defined on the basis of sequence homology and on the presence of variations on a conserved cysteine motif, which allows the family to further divide into four subfamilies (CC, CXC, XC, and CX3C). Chemokines interact with seven-transmembrane receptors which are typically coupled to G protein for signaling. Currently, there are ten known receptors for CC chemokines, seven for CXC chemokines, and single receptors for the XC and CX3C chemokines. In addition to these classical chemokine receptors, there exists a subfamily of atypical chemokine receptors (ACKRs) that are unable to couple to G-proteins and, instead, they preferentially mediate beta-arrestin dependent processes, such as receptor internalization, after ligand binding. The classical chemokine receptors contain a conserved DRYLAIV motif in the second intracellular loop, which is required for G-protein coupling. However, the ACKRs lack this conserved motif and fail to couple to G-proteins and induce classical GPCR signaling. Five receptors have been identified for the ACKR family, including CC-chemokine receptors like 1 and 2 (CCRL1 and CCRL2), CXCR7, Duffy antigen receptor for chemokine (DARC), and D6. Both ACKR1 (DARC) and ACKR3 (CXCR7) show low sequence homology to the classic chemokine receptors. Pssm-ID: 341319 [Multi-domain] Cd Length: 278 Bit Score: 72.63 E-value: 1.36e-14
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| 7tmA_Trissin_R | cd15012 | trissin receptor and related proteins, member of the class A family of seven-transmembrane G ... |
80-327 | 1.45e-14 | |||||
trissin receptor and related proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This subgroup represents the Drosophila melanogaster trissin receptor and closely related invertebrate proteins which are a member of the class A family of seven-transmembrane G-protein coupled receptors. The cysteine-rich trissin has been shown to be an endogenous ligand for the orphan CG34381 in Drosophila melanogaster. Trissin is a peptide composed of 28 amino acids with three intrachain disulfide bonds with no significant structural similarities to known endogenous peptides. Cysteine-rich peptides are known to have antimicrobial or toxicant activities, although frequently their mechanism of action is poorly understood. Since the expression of trissin and its receptor is reported to predominantly localize to the brain and thoracicoabdominal ganglion, trissin is predicted to behave as a neuropeptide. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320140 [Multi-domain] Cd Length: 277 Bit Score: 72.48 E-value: 1.45e-14
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| 7tmA_tyramine_R-like | cd15061 | tyramine receptors and similar proteins, member of the class A family of seven-transmembrane G ... |
78-327 | 3.82e-14 | |||||
tyramine receptors and similar proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes tyramine-specific receptors and similar proteins found in insects and other invertebrates. These tyramine receptors form a distinct receptor family that is phylogenetically different from the other tyramine/octopamine receptors which also found in invertebrates. Both octopamine and tyramine mediate their actions via G protein-coupled receptors (GPCRs) and are the invertebrate equivalent of vertebrate adrenergic neurotransmitters. In Drosophila, octopamine is involved in ovulation by mediating an egg release from the ovary, while a physiological role for tyramine in this process is not fully understood. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320189 [Multi-domain] Cd Length: 256 Bit Score: 71.24 E-value: 3.82e-14
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| PHA03087 | PHA03087 | G protein-coupled chemokine receptor-like protein; Provisional |
39-327 | 4.96e-14 | |||||
G protein-coupled chemokine receptor-like protein; Provisional Pssm-ID: 222976 [Multi-domain] Cd Length: 335 Bit Score: 71.73 E-value: 4.96e-14
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| 7tmA_SSTR4 | cd15973 | somatostatin receptor type 4, member of the class A family of seven-transmembrane G ... |
106-327 | 5.68e-14 | |||||
somatostatin receptor type 4, member of the class A family of seven-transmembrane G protein-coupled receptors; G protein-coupled somatostatin receptors (SSTRs) are composed of five distinct subtypes (SSTR1-5) that display strong sequence similarity with opioid receptors. All five receptor subtypes bind the natural somatostatin (somatotropin release inhibiting factor), a polypeptide hormone that regulates a wide variety of physiological functions such as neurotransmission, cell proliferation, contractility of smooth muscle cells, and endocrine signaling as well as inhibition of the release of many secondary hormones. SSTR4 plays a critical role in mediating inflammation. Unlike other SSTRs, SSTR4 subtype is not detected in all pituitary adenomas while it is expressed in the normal human pituitary. Pssm-ID: 320639 [Multi-domain] Cd Length: 274 Bit Score: 71.04 E-value: 5.68e-14
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| 7tmA_capaR | cd15134 | neuropeptide capa receptor and similar invertebrate proteins, member of the class A family of ... |
107-328 | 8.15e-14 | |||||
neuropeptide capa receptor and similar invertebrate proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; CapaR is a G-protein coupled receptor for the Drosophila melanogaster capa neuropeptides (Drm-capa-1 and -2), which act on the Malpighian tubules to increase fluid transport. The capa peptides are evolutionarily related to vertebrate Neuromedin U neuropeptide and contain a C-terminal FPRXamide motif. CapaR regulates fluid homeostasis through its ligands, thereby acts as a desiccation stress-responsive receptor. CapaR undergoes desensitization, with internalization mediated by beta-arrestin-2. Pssm-ID: 320262 [Multi-domain] Cd Length: 298 Bit Score: 70.82 E-value: 8.15e-14
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| 7tmA_MCHR-like | cd15088 | melanin concentrating hormone receptor, member of the class A family of seven-transmembrane G ... |
83-327 | 9.96e-14 | |||||
melanin concentrating hormone receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; Melanin-concentrating hormone receptor (MCHR) binds melanin concentrating hormone and is presumably involved in the neuronal regulation of food intake and energy homeostasis. Despite strong homology with somatostatin receptors, MCHR does not appear to bind somatostatin. Two MCHRs have been characterized in vertebrates, MCHR1 and MCHR2. MCHR1 is expressed in all mammals, whereas MCHR2 is only expressed in the higher order mammals, such as humans, primates, and dogs, and is not found in rodents. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320216 [Multi-domain] Cd Length: 278 Bit Score: 70.17 E-value: 9.96e-14
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| 7tmA_GPR33 | cd15120 | orphan receptor GPR33, member of the class A family of seven-transmembrane G protein-coupled ... |
78-323 | 1.12e-13 | |||||
orphan receptor GPR33, member of the class A family of seven-transmembrane G protein-coupled receptors; G-protein coupled receptor GPR33, an orphan member of the chemokine-like receptor family, was originally identified as a pseudogene in humans as well as in several apes and rodent species. Although the intact GPR33 allele is still present in a small fraction of the human population, the human GPR33 contains a premature stop codon. The amino acid sequence of GPR33 shares a high degree of sequence identity with the members of the chemokine and chemoattractant receptors that control leukocyte chemotaxis. The human GPR33 is expressed in spleen, lung, heart, kidney, pancreas, thymus, gonads, and leukocytes. Pssm-ID: 320248 [Multi-domain] Cd Length: 282 Bit Score: 70.20 E-value: 1.12e-13
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| 7tmA_Proton-sensing_R | cd15160 | proton-sensing G protein-coupled receptors, member of the class A family of ... |
80-323 | 1.14e-13 | |||||
proton-sensing G protein-coupled receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Proton/pH-sensing G-protein coupled receptors sense pH of 7.6 to 6.0. They mediate a variety of biological activities in neutral and mildly acidic pH conditions, whereas the acid-sensing ionotropic ion channels typically sense strong acidic pH. The proton/pH-sensing receptor family includes the G2 accumulation receptor (G2A, also known as GPR132), the T cell death associated gene-8 (TDAG8, GPR65) receptor, ovarian cancer G-protein receptor 1 (OGR-1, GPR68), and G-protein-coupled receptor 4 (GPR4). Pssm-ID: 320288 [Multi-domain] Cd Length: 280 Bit Score: 70.11 E-value: 1.14e-13
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| 7tmA_CCK-BR | cd15979 | cholecystokinin receptor type B, member of the class A family of seven-transmembrane G ... |
80-323 | 1.39e-13 | |||||
cholecystokinin receptor type B, member of the class A family of seven-transmembrane G protein-coupled receptors; Cholecystokinin receptors (CCK-AR and CCK-BR) are a group of G-protein coupled receptors which bind the peptide hormones cholecystokinin (CCK) or gastrin. CCK, which facilitates digestion in the small intestine, and gastrin, a major regulator of gastric acid secretion, are highly similar peptides. Like gastrin, CCK is a naturally-occurring linear peptide that is synthesized as a preprohormone, then proteolytically cleaved to form a family of peptides with the common C-terminal sequence (Gly-Trp-Met-Asp-Phe-NH2), which is required for full biological activity. CCK-AR (type A, alimentary; also known as CCK1R) is found abundantly on pancreatic acinar cells and binds only sulfated CCK-peptides with very high affinity, whereas CCK-BR (type B, brain; also known as CCK2R), the predominant form in the brain and stomach, binds CCK or gastrin and discriminates poorly between sulfated and non-sulfated peptides. CCK is implicated in regulation of digestion, appetite control, and body weight, and is involved in neurogenesis via CCK-AR. There is some evidence to support that CCK and gastrin, via their receptors, are involved in promoting cancer development and progression, acting as growth and invasion factors. Pssm-ID: 320645 [Multi-domain] Cd Length: 275 Bit Score: 69.84 E-value: 1.39e-13
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| 7tmA_NTSR-like | cd14979 | neurotensin receptors and related G protein-coupled receptors, member of the class A family of ... |
80-323 | 1.95e-13 | |||||
neurotensin receptors and related G protein-coupled receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; This subfamily includes the neurotensin receptors and related G-protein coupled receptors, including neuromedin U receptors, growth hormone secretagogue receptor, motilin receptor, the putative GPR39 and the capa receptors from insects. These receptors all bind peptide hormones with diverse physiological effects. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320110 [Multi-domain] Cd Length: 300 Bit Score: 69.69 E-value: 1.95e-13
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| 7tmA_CXCR1_2 | cd15178 | CXC chemokine receptor types 1 and 2, member of the class A family of seven-transmembrane G ... |
80-285 | 2.52e-13 | |||||
CXC chemokine receptor types 1 and 2, member of the class A family of seven-transmembrane G protein-coupled receptors; CXCR1 and CXCR2 are closely related chemotactic receptors for a group of CXC chemokines distinguished by the presence of the amino acid motif ELR immediately adjacent to their CXC motif. Expression of CXCR1 and CXCR2 is strictly controlled in neutrophils by external stimuli such as lipopolysaccharide (LPS), tumor necrosis factor (TNF)-alpha, Toll-like receptor agonists, and nitric oxide. CXCL8 (formerly known as interleukin-8) binds with high-affinity and activates both receptors. CXCR1 also binds CXCL7 (neutrophil-activating protein-2), whereas CXCR2 non-selectively binds to all seven ELR-positive chemokines (CXCL1-7). Chemokines are principal regulators for leukocyte trafficking, recruitment, and activation. Chemokine family membership is defined on the basis of sequence homology and on the presence of variations on a conserved cysteine motif, which allows the family to further divide into four subfamilies (CC, CXC, XC, and CX3C). Chemokines interact with seven-transmembrane receptors which are typically coupled to G protein for signaling. Currently, there are ten known receptors for CC chemokines, seven for CXC chemokines, and single receptors for the XC and CX3C chemokines. Pssm-ID: 341333 [Multi-domain] Cd Length: 279 Bit Score: 69.22 E-value: 2.52e-13
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| 7tmA_KiSS1R | cd15095 | KiSS1-derived peptide (kisspeptin) receptor, member of the class A family of ... |
104-326 | 2.76e-13 | |||||
KiSS1-derived peptide (kisspeptin) receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; The G protein-coupled KiSS1-derived peptide receptor (GPR54 or kisspeptin receptor) binds the peptide hormone kisspeptin (previously known as metastin), which encoded by the metastasis suppressor gene (KISS1) expressed in various endocrine and reproductive tissues. The KiSS1 receptor is coupled to G proteins of the G(q/11) family, which lead to activation of phospholipase C and increase of intracellular calcium. This signaling cascade plays an important role in reproduction by regulating the secretion of gonadotropin-releasing hormone. Pssm-ID: 320223 [Multi-domain] Cd Length: 288 Bit Score: 68.85 E-value: 2.76e-13
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| 7tmA_FMRFamide_R-like | cd14978 | FMRFamide (Phe-Met-Arg-Phe) receptors and related proteins, member of the class A family of ... |
113-327 | 3.65e-13 | |||||
FMRFamide (Phe-Met-Arg-Phe) receptors and related proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes Drosophila melanogaster G-protein coupled FMRFamide (Phe-Met-Arg-Phe-NH2) receptor DrmFMRFa-R and related invertebrate receptors, as well as the vertebrate proteins GPR139 and GPR142. DrmFMRFa-R binds with high affinity to FMRFamide and intrinsic FMRFamide-related peptides. FMRFamide is a neuropeptide from the family of FMRFamide-related peptides (FaRPs), which all containing a C-terminal RFamide (Arg-Phe-NH2) motif and have diverse functions in the central and peripheral nervous systems. FMRFamide is an important neuropeptide in many types of invertebrates such as insects, nematodes, molluscs, and worms. In invertebrates, the FMRFamide-related peptides are involved in the regulation of heart rate, blood pressure, gut motility, feeding behavior, and reproduction. On the other hand, in vertebrates such as mice, they play a role in the modulation of morphine-induced antinociception. Orphan receptors GPR139 and GPR142 are very closely related G protein-coupled receptors, but they have different expression patterns in the brain and in other tissues. These receptors couple to inhibitory G proteins and activate phospholipase C. Studies suggested that dimer formation may be required for their proper function. GPR142 is predominantly expressed in pancreatic beta-cells and mediates enhancement of glucose-stimulated insulin secretion, whereas GPR139 is mostly expressed in the brain and is suggested to play a role in the control of locomotor activity. Tryptophan and phenylalanine have been identified as putative endogenous ligands of GPR139. Pssm-ID: 410630 [Multi-domain] Cd Length: 299 Bit Score: 68.81 E-value: 3.65e-13
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| 7tmA_Beta_AR | cd15058 | beta adrenergic receptors (adrenoceptors), member of the class A family of seven-transmembrane ... |
83-323 | 5.14e-13 | |||||
beta adrenergic receptors (adrenoceptors), member of the class A family of seven-transmembrane G protein-coupled receptors; The beta adrenergic receptor (beta adrenoceptor), also known as beta AR, is activated by hormone adrenaline (epinephrine) and plays important roles in regulating cardiac function and heart rate, as well as pulmonary physiology. The human heart contains three subtypes of the beta AR: beta-1 AR, beta-2 AR, and beta-3 AR. Beta-1 AR and beta-2 AR, which expressed at about a ratio of 70:30, are the major subtypes involved in modulating cardiac contractility and heart rate by positively stimulating the G(s) protein-adenylate cyclase-cAMP-PKA signaling pathway. In contrast, beta-3 AR produces negative inotropic effects by activating inhibitory G(i) proteins. The aberrant expression of beta-ARs can lead to cardiac dysfunction such as arrhythmias or heart failure. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320186 [Multi-domain] Cd Length: 305 Bit Score: 68.63 E-value: 5.14e-13
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| 7tmA_leucokinin-like | cd15393 | leucokinin-like peptide receptor from tick and related proteins, member of the class A family ... |
106-327 | 1.27e-12 | |||||
leucokinin-like peptide receptor from tick and related proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This subgroup includes a leucokinin-like peptide receptor from the Southern cattle tick, Boophilus microplus, a pest of cattle world-wide. Leucokinins are invertebrate neuropeptides that exhibit myotropic and diuretic activity. This receptor is the first neuropeptide receptor known from the Acari and the second known in the subfamily of leucokinin-like peptide G-protein-coupled receptors. The other known leucokinin-like peptide receptor is a lymnokinin receptor from the mollusc Lymnaea stagnalis. Pssm-ID: 320515 [Multi-domain] Cd Length: 288 Bit Score: 67.05 E-value: 1.27e-12
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| 7tmA_ET_R-like | cd14977 | endothelin receptors and related proteins, member of the class A family of seven-transmembrane ... |
79-322 | 1.34e-12 | |||||
endothelin receptors and related proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This subfamily of G-protein coupled receptors includes endothelin receptors, bombesin receptor subtype 3 (BRS-3), gastrin-releasing peptide receptor (GRPR), neuromedin B receptor (NMB-R), endothelin B receptor-like 2 (ETBR-LP-2), and GRP37. The endothelin receptors and related proteins are members of the seven transmembrane rhodopsin-like G-protein coupled receptor family (class A GPCRs) which activate multiple effectors via different types of G protein. Pssm-ID: 320108 [Multi-domain] Cd Length: 292 Bit Score: 67.06 E-value: 1.34e-12
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| 7tmA_CMKLR1 | cd15116 | chemokine-like receptor 1, member of the class A family of seven-transmembrane G ... |
107-323 | 1.43e-12 | |||||
chemokine-like receptor 1, member of the class A family of seven-transmembrane G protein-coupled receptors; Chemokine receptor-like 1 (also known as Chemerin receptor 23) is a GPCR for the chemoattractant adipokine chemerin, also known as retinoic acid receptor responder protein 2 (RARRES2), and for the omega-3 fatty acid derived molecule resolvin E1. Interaction with chemerin induces activation of the MAPK and PI3K signaling pathways leading to downstream functional effects, such as a decrease in immune responses, stimulation of adipogenesis, and angiogenesis. On the other hand, resolvin E1 negatively regulates the cytokine production in macrophages by reducing the activation of MAPK1/3 and NF-kB pathways. CMKLR1 is prominently expressed in dendritic cells and macrophages. Pssm-ID: 320244 [Multi-domain] Cd Length: 284 Bit Score: 67.10 E-value: 1.43e-12
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| 7tmA_Delta_opioid_R | cd15089 | opioid receptor subtype delta, member of the class A family of seven-transmembrane G ... |
82-326 | 1.47e-12 | |||||
opioid receptor subtype delta, member of the class A family of seven-transmembrane G protein-coupled receptors; The delta-opioid receptor binds the endogenous pentapeptide ligands such as enkephalins and produces antidepressant-like effects. The opioid receptor family is composed of four major subtypes: mu (MOP), delta (DOP), kappa (KOP) opioid receptors, and the nociceptin/orphanin FQ peptide receptor (NOP). They are distributed widely in the central nervous system and respond to classic alkaloid opiates, such as morphine and heroin, as well as to endogenous peptide ligands, which include dynorphins, enkephalins, endorphins, endomorphins, and nociceptin. Opioid receptors are coupled to inhibitory G proteins of the G(i/o) family and involved in regulating a variety of physiological functions such as pain, addiction, mood, stress, epileptic seizure, and obesity, among many others. Pssm-ID: 320217 [Multi-domain] Cd Length: 281 Bit Score: 66.90 E-value: 1.47e-12
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| 7tmA_5-HT1A_invertebrates | cd15331 | serotonin receptor subtype 1A from invertebrates, member of the class A family of ... |
79-327 | 1.54e-12 | |||||
serotonin receptor subtype 1A from invertebrates, member of the class A family of seven-transmembrane G protein-coupled receptors; The 5-HT1 receptors, one of 14 mammalian 5-HT receptors, is a member of the class A of GPCRs and is activated by the endogenous neurotransmitter and peripheral signal mediator serotonin (5-hydroxytryptamine, 5-HT). The 5-HT1 receptors mediate inhibitory neurotransmission by coupling to G proteins of the G(i/o) family, which lead to a decrease in adenylate cyclase activity, thereby decreasing intracellular cAMP levels and calcium influx. The 5-HT1 receptor subfamily includes 5 subtypes: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F. There is no 5-HT1C receptor subtype, as it has been reclassified as the 5-HT2C receptor. In the CNS, serotonin is involved in the regulation of appetite, mood, sleep, cognition, learning and memory, as well as implicated in neurologic disorders such as migraine, schizophrenia, and depression. Pssm-ID: 320454 [Multi-domain] Cd Length: 261 Bit Score: 66.61 E-value: 1.54e-12
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| 7tmA_GPR19 | cd15008 | G protein-coupled receptor 19, member of the class A family of seven-transmembrane G ... |
83-290 | 1.66e-12 | |||||
G protein-coupled receptor 19, member of the class A family of seven-transmembrane G protein-coupled receptors; G-protein coupled receptor 19 is an orphan receptor that is expressed predominantly in neuronal cells during mouse embryogenesis. Its mRNA is found frequently over-expressed in patients with small cell lung cancer. GPR19 shares a significant amino acid sequence identity with the D2 dopamine and neuropeptide Y families of receptors. Human GPR19 gene, intronless in the coding region, also has a distribution in brain overlapping that of the D2 dopamine receptor gene, and is located on chromosome 12. GPR19 is a member of the class A family of GPCRs, which represents a widespread protein family that includes the light-sensitive rhodopsin as well as receptors for biogenic amines, lipids, nucleotides, odorants, peptide hormones, and a variety of other ligands. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320137 [Multi-domain] Cd Length: 275 Bit Score: 66.78 E-value: 1.66e-12
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| 7tmA_Octopamine_R | cd15063 | octopamine receptors in invertebrates, member of the class A family of seven-transmembrane G ... |
78-327 | 1.66e-12 | |||||
octopamine receptors in invertebrates, member of the class A family of seven-transmembrane G protein-coupled receptors; G-protein coupled receptor for octopamine (OA), which functions as a neurotransmitter, neurohormone, and neuromodulator in invertebrate nervous system. Octopamine (also known as beta, 4-dihydroxyphenethylamine) is an endogenous trace amine that is highly similar to norepinephrine, but lacks a hydroxyl group, and has effects on the adrenergic and dopaminergic nervous systems. Based on the pharmacological and signaling profiles, the octopamine receptors can be classified into at least two groups: OA1 receptors elevate intracellular calcium levels in muscle, whereas OA2 receptors activate adenylate cyclase and increase cAMP production. Pssm-ID: 320191 [Multi-domain] Cd Length: 266 Bit Score: 66.37 E-value: 1.66e-12
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| 7tmA_TAAR5 | cd15318 | trace amine-associated receptor 5, member of the class A family of seven-transmembrane G ... |
78-326 | 2.21e-12 | |||||
trace amine-associated receptor 5, member of the class A family of seven-transmembrane G protein-coupled receptors; The trace amine-associated receptor 5 is one of the 15 identified amine-activated G protein-coupled receptors (TAARs), a distinct subfamily within the class A G protein-coupled receptors. Trace amines are endogenous amines of unknown function that have strong structural and metabolic similarity to classical monoamine neurotransmitters (serotonin, noradrenaline, adrenaline, dopamine, and histamine), which play critical roles in human and animal physiological activities such as cognition, consciousness, mood, motivation, perception, and autonomic responses. However, trace amines are found in the mammalian brain at very low concentrations compared to classical monoamines. Trace amines, including p-tyramine, beta-phenylethylamine, and tryptamine, are also thought to act as chemical messengers to exert their biological effects in vertebrates. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320441 [Multi-domain] Cd Length: 282 Bit Score: 66.42 E-value: 2.21e-12
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| 7tmA_PAR | cd15162 | protease-activated receptors, member of the class A family of seven-transmembrane G ... |
69-327 | 2.66e-12 | |||||
protease-activated receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; This subfamily includes purinergic receptor P2Y8 and protease-activated receptors. P2Y8 (or P2RY8) expression is often increased in leukemia patients, and it plays a role in the pathogenesis of acute leukemia. P2Y8 is phylogenetically closely related to the protease-activated receptors (PARs), which are activated by serine proteases such as thrombin, trypsin, and tryptase. These proteases cleave the extracellular domain of the receptor to form a new N-terminus, which in turn functions as a tethered ligand. The newly-formed tethered ligand binds intramolecularly to activate the receptor and triggers G-protein binding and intracellular signaling. Four different types of the protease-activated receptors have been identified (PAR1-4) and are predominantly expressed in platelets. PAR1, PAR3, and PAR4 are activated by thrombin, whereas PAR2 is activated by trypsin. The PARs are known to couple with several G-proteins including Gi (cAMP inhibitory), G12/13 (Rho and Ras activation), and Gq (calcium signaling) to activate downstream signaling messengers which induces numerous cellular and physiological effects. Pssm-ID: 341328 [Multi-domain] Cd Length: 280 Bit Score: 65.93 E-value: 2.66e-12
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| 7tmA_D1-like_dopamine_R | cd15057 | D1-like family of dopamine receptors, member of the class A family of seven-transmembrane G ... |
83-325 | 2.71e-12 | |||||
D1-like family of dopamine receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Dopamine receptors are members of the class A G protein-coupled receptors that are involved in many neurological processes in the central nervous system (CNS). The neurotransmitter dopamine is the primary endogenous agonist for dopamine receptors. Dopamine receptors consist of at least five subtypes: D1, D2, D3, D4, and D5. The D1 and D5 subtypes are members of the D1-like family of dopamine receptors, whereas the D2, D3 and D4 subtypes are members of the D2-like family. The D1-like family receptors are coupled to G proteins of the G(s) family, which activate adenylate cyclase, causing cAMP formation and activation of protein kinase A. In contrast, activation of D2-like family receptors is linked to G proteins of the G(i) family, which inhibit adenylate cyclase. Dopamine receptors are major therapeutic targets for neurological and psychiatric disorders such as drug abuse, depression, schizophrenia, or Parkinson's disease. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320185 [Multi-domain] Cd Length: 299 Bit Score: 66.30 E-value: 2.71e-12
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| 7tmA_NPY6R | cd15396 | neuropeptide Y receptor type 6, member of the class A family of seven-transmembrane G ... |
78-327 | 2.86e-12 | |||||
neuropeptide Y receptor type 6, member of the class A family of seven-transmembrane G protein-coupled receptors; NPY is a 36-amino acid peptide neurotransmitter with a C-terminal tyrosine amide residue that is widely distributed in the brain and the autonomic nervous system of many mammalian species. NPY exerts its functions through five, G-protein coupled receptor subtypes including NPY1R, NPY2R, NPY4R, NPY5R, and NPY6R; however, NPY6R is not functional in humans. NYP receptors are also activated by its two other family members, peptide YY (PYY) and pancreatic polypeptide (PP). They typically couple to G(i) or G(o) proteins, which leads to a decrease in adenylate cyclase activity, thereby decreasing intracellular cAMP levels, and are involved in diverse physiological roles including appetite regulation, circadian rhythm, and anxiety. Pssm-ID: 320518 [Multi-domain] Cd Length: 293 Bit Score: 66.01 E-value: 2.86e-12
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| 7tmA_AT1R | cd15192 | type 1 angiotensin II receptor, member of the class A family of seven-transmembrane G ... |
106-326 | 3.04e-12 | |||||
type 1 angiotensin II receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; Angiotensin II (Ang II), the main effector in the renin-angiotensin system, plays a crucial role in the regulation of cardiovascular homeostasis through its type 1 (AT1) and type 2 (AT2) receptors. Ang II contributes to cardiovascular diseases such as hypertension and atherosclerosis via AT1R activation. Ang II increases blood pressure through Gq-mediated activation of phospholipase C, resulting in phosphoinositide (PI) hydrolysis and increased intracellular calcium levels. Through the AT2R, Ang II counteracts the vasoconstrictor action of AT1R and thereby induces vasodilation, sodium excretion, and reduction of blood pressure. Moreover, AT1R promotes cell proliferation, whereas AT2R inhibits proliferation and stimulates cell differentiation. The AT2R is highly expressed during fetal development, however it is scarcely present in adult tissues and is induced in pathological conditions. Generally, the AT1R mediates many actions of Ang II, while the AT2R is involved in the regulation of blood pressure and renal function. Pssm-ID: 320320 [Multi-domain] Cd Length: 285 Bit Score: 65.92 E-value: 3.04e-12
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| 7tmA_D2-like_dopamine_R | cd15053 | D2-like dopamine receptors, member of the class A family of seven-transmembrane G ... |
83-326 | 4.33e-12 | |||||
D2-like dopamine receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Dopamine receptors are members of the class A G protein-coupled receptors that are involved in many neurological processes in the central nervous system (CNS). The neurotransmitter dopamine is the primary endogenous agonist for dopamine receptors. Dopamine receptors consist of at least five subtypes: D1, D2, D3, D4, and D5. The D1 and D5 subtypes are members of the D1-like family of dopamine receptors, whereas the D2, D3 and D4 subtypes are members of the D2-like family. The D1-like family receptors are coupled to G proteins of the G(s) family, which activate adenylate cyclase, causing cAMP formation and activation of protein kinase A. In contrast, activation of D2-like family receptors is linked to G proteins of the G(i) family, which inhibit adenylate cyclase. Dopamine receptors are major therapeutic targets for neurological and psychiatric disorders such as drug abuse, depression, schizophrenia, or Parkinson's disease. Pssm-ID: 320181 [Multi-domain] Cd Length: 263 Bit Score: 65.06 E-value: 4.33e-12
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| 7tmA_LTB4R2 | cd15122 | leukotriene B4 receptor subtype 2 (LTB4R2 or BLT2), member of the class A family of ... |
67-325 | 5.47e-12 | |||||
leukotriene B4 receptor subtype 2 (LTB4R2 or BLT2), member of the class A family of seven-transmembrane G protein-coupled receptors; Leukotriene B4 (LTB4), a metabolite of arachidonic acid, is a powerful chemotactic activator for granulocytes and macrophages. Two receptors for LTB4 have been identified: a high-affinity receptor (LTB4R1 or BLT1) and a low-affinity receptor (TB4R2 or BLT2). Both BLT1 and BLT2 receptors belong to the rhodopsin-like G-protein coupled receptor superfamily and primarily couple to G(i) proteins, which lead to chemotaxis, calcium mobilization, and inhibition of adenylate cyclase. In some cells, they can also couple to the Gq-like protein, G16, and activate phospholipase C. LTB4 is involved in mediating inflammatory processes, immune responses, and host defense against infection. Studies have shown that LTB4 stimulates leukocyte extravasation, neutrophil degranulation, lysozyme release, and reactive oxygen species generation. Pssm-ID: 320250 [Multi-domain] Cd Length: 281 Bit Score: 65.21 E-value: 5.47e-12
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| 7tmA_NPFFR2 | cd15980 | neuropeptide FF receptor 2, member of the class A family of seven-transmembrane G ... |
78-327 | 7.04e-12 | |||||
neuropeptide FF receptor 2, member of the class A family of seven-transmembrane G protein-coupled receptors; Neuropeptide FF (NPFF) is a mammalian octapeptide that belongs to a family of neuropeptides containing an RF-amide motif at their C-terminus that have been implicated in a wide range of physiological functions in the brain including pain sensitivity, insulin release, food intake, memory, blood pressure, and opioid-induced tolerance and hyperalgesia. The effects of these peptides are mediated through neuropeptide FF1 and FF2 receptors (NPFF1-R and NPFF2-R) which are predominantly expressed in the brain. NPFF induces pro-nociceptive effects, mainly through the NPFF1-R, and anti-nociceptive effects, mainly through the NPFF2-R. NPFF has been shown to inhibit adenylate cyclase via the Gi protein coupled to NPFF1-R. Pssm-ID: 320646 [Multi-domain] Cd Length: 299 Bit Score: 64.91 E-value: 7.04e-12
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| 7tmA_SKR_NK2R | cd16004 | substance-K receptor, member of the class A family of seven-transmembrane G protein-coupled ... |
107-323 | 1.42e-11 | |||||
substance-K receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; The substance-K receptor (SKR), also known as tachykinin receptor 2 (TACR2) or neurokinin A receptor or NK2R, is a G-protein coupled receptor that specifically binds to neurokinin A. The tachykinins are widely distributed throughout the mammalian central and peripheral nervous systems and act as excitatory transmitters on neurons and cells in the gastrointestinal tract. The TKs are characterized by a common five-amino acid C-terminal sequence, Phe-X-Gly-Leu-Met-NH2, where X is a hydrophobic residue. The three major mammalian tachykinins are substance P (SP), neurokinin A (NKA), and neurokinin B (NKB). The physiological actions of tachykinins are mediated through three types of receptors: neurokinin receptor type 1 (NK1R), NK2R, and NK3R. SP is a high-affinity endogenous ligand for NK1R, which interacts with the Gq protein and activates phospholipase C, leading to elevation of intracellular calcium. NK2R is a high-affinity receptor for NKA, the tachykinin neuropeptide substance K. SP and NKA are found in the enteric nervous system and mediate the regulation of gastrointestinal motility, secretion, vascular permeability, and pain perception. Pssm-ID: 320670 [Multi-domain] Cd Length: 285 Bit Score: 64.09 E-value: 1.42e-11
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| 7tmA_Kappa_opioid_R | cd15091 | opioid receptor subtype kappa, member of the class A family of seven-transmembrane G ... |
82-326 | 1.45e-11 | |||||
opioid receptor subtype kappa, member of the class A family of seven-transmembrane G protein-coupled receptors; The kappa-opioid receptor binds the opioid peptide dynorphin as the primary endogenous ligand. The opioid receptor family is composed of four major subtypes: mu (MOP), delta (DOP), kappa (KOP) opioid receptors, and the nociceptin/orphanin FQ peptide receptor (NOP). They are distributed widely in the central nervous system and respond to classic alkaloid opiates, such as morphine and heroin, as well as to endogenous peptide ligands, which include dynorphins, enkephalins, endorphins, endomorphins, and nociceptin. Opioid receptors are coupled to inhibitory G proteins of the G(i/o) family and involved in regulating a variety of physiological functions such as pain, addiction, mood, stress, epileptic seizure, and obesity, among many others. Pssm-ID: 320219 [Multi-domain] Cd Length: 282 Bit Score: 63.82 E-value: 1.45e-11
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| 7tmA_tyramine_octopamine_R-like | cd15060 | tyramine/octopamine receptor-like, member of the class A family of seven-transmembrane G ... |
83-328 | 1.56e-11 | |||||
tyramine/octopamine receptor-like, member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes tyramine/octopamine receptors and similar proteins found in insects and other invertebrates. Both octopamine and tyramine mediate their actions via G protein-coupled receptors (GPCRs) and are the invertebrate equivalent of vertebrate adrenergic neurotransmitters. In Drosophila, octopamine is involved in ovulation by mediating an egg release from the ovary, while a physiological role for tyramine in this process is not fully understood. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320188 [Multi-domain] Cd Length: 260 Bit Score: 63.60 E-value: 1.56e-11
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| 7tmA_Mu_opioid_R | cd15090 | opioid receptor subtype mu, member of the class A family of seven-transmembrane G ... |
82-326 | 1.90e-11 | |||||
opioid receptor subtype mu, member of the class A family of seven-transmembrane G protein-coupled receptors; The mu-opioid receptor binds endogenous opioids such as beta-endorphin and endomorphin. The opioid receptor family is composed of four major subtypes: mu (MOP), delta (DOP), kappa (KOP) opioid receptors, and the nociceptin/orphanin FQ peptide receptor (NOP). They are distributed widely in the central nervous system and respond to classic alkaloid opiates, such as morphine and heroin, as well as to endogenous peptide ligands, which include dynorphins, enkephalins, endorphins, endomorphins, and nociceptin. Opioid receptors are coupled to inhibitory G proteins of the G(i/o) family and involved in regulating a variety of physiological functions such as pain, addiction, mood, stress, epileptic seizure, and obesity, among many others. Pssm-ID: 320218 [Multi-domain] Cd Length: 279 Bit Score: 63.47 E-value: 1.90e-11
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| 7tmA_CXCR3 | cd15180 | CXC chemokine receptor type 3, member of the class A family of seven-transmembrane G ... |
73-327 | 2.19e-11 | |||||
CXC chemokine receptor type 3, member of the class A family of seven-transmembrane G protein-coupled receptors; CXCR3 is an inflammatory chemotactic receptor for a group of CXC chemokines distinguished by the presence of the amino acid motif ELR immediately adjacent to their CXC motif. CXCR3 specifically binds three chemokines CXCL9 (monokine induced by gamma-interferon), CXCL10 (interferon induced protein of 10 kDa), and CXCL11 (interferon inducible T-cell alpha-chemoattractant, I-TAC). CXC3R is expressed on CD4+ Th1 and CD8+ cytotoxic T lymphocytes as well as highly on innate lymphocytes, such as NK cells and NK T cells, where it may mediate the recruitment of these cells to the sites of infection and inflammation. Chemokines are principal regulators for leukocyte trafficking, recruitment, and activation. Chemokine family membership is defined on the basis of sequence homology and on the presence of variations on a conserved cysteine motif, which allows the family to further divide into four subfamilies (CC, CXC, XC, and CX3C). Chemokines interact with seven-transmembrane receptors which are typically coupled to G protein for signaling. Currently, there are ten known receptors for CC chemokines, seven for CXC chemokines, and single receptors for the XC and CX3C chemokines. Pssm-ID: 341335 [Multi-domain] Cd Length: 280 Bit Score: 63.56 E-value: 2.19e-11
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| 7tmA_alpha2_AR | cd15059 | alpha-2 adrenergic receptors, member of the class A family of seven-transmembrane G ... |
78-326 | 2.77e-11 | |||||
alpha-2 adrenergic receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; The alpha-2 adrenergic receptors (or adrenoceptors) are a subfamily of the class A rhodopsin-like GPCRs that share a common architecture of seven transmembrane helices. This subfamily consists of three highly homologous receptor subtypes that have a key role in neurotransmitter release: alpha-2A, alpha-2B, and alpha-2C. In addition, a fourth subtype, alpha-2D is present in ray-finned fishes and amphibians, but is not found in humans. The alpha-2 receptors are found in both central and peripheral nervous system and serve to produce inhibitory functions through the G(i) proteins. Thus, the alpha-2 receptors inhibit adenylate cyclase, which decreases cAMP production and thereby decreases calcium influx during the action potential. Consequently, lowered levels of calcium will lead to a decrease in neurotransmitter release by negative feedback. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320187 [Multi-domain] Cd Length: 261 Bit Score: 62.74 E-value: 2.77e-11
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| 7tmA_SSTR | cd15093 | somatostatin receptors, member of the class A family of seven-transmembrane G protein-coupled ... |
95-327 | 2.82e-11 | |||||
somatostatin receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; G protein-coupled somatostatin receptors (SSTRs) are composed of five distinct subtypes (SSTR1-5) that display strong sequence similarity with opioid receptors. All five receptor subtypes bind the natural somatostatin (somatotropin release inhibiting factor), a polypeptide hormone that regulates a wide variety of physiological functions such as neurotransmission, cell proliferation, contractility of smooth muscle cells, and endocrine signaling as well as inhibition of the release of many secondary hormones. They share common signaling cascades such as inhibition of adenylyl cyclase, activation of phosphotyrosine phosphatase activity, and G-protein-dependent regulation of MAPKs. Pssm-ID: 320221 [Multi-domain] Cd Length: 280 Bit Score: 63.25 E-value: 2.82e-11
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| 7tmA_NKR_NK3R | cd16003 | neuromedin-K receptor, member of the class A family of seven-transmembrane G protein-coupled ... |
106-288 | 3.60e-11 | |||||
neuromedin-K receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; The neuromedin-K receptor (NKR), also known as tachykinin receptor 3 (TACR3) or neurokinin B receptor or NK3R, is a G-protein coupled receptor that specifically binds to neurokinin B. The tachykinins (TKs) act as excitatory transmitters on neurons and cells in the gastrointestinal tract. The TKs are characterized by a common five-amino acid C-terminal sequence, Phe-X-Gly-Leu-Met-NH2, where X is a hydrophobic residue. The three major mammalian tachykinins are substance P (SP), neurokinin A (NKA), and neurokinin B (NKB). The physiological actions of tachykinins are mediated through three types of receptors: neurokinin receptor type 1 (NK1R), NK2R, and NK3R. NK3R is activated by its high-affinity ligand, NKB, which is primarily involved in the central nervous system and plays a critical role in the regulation of gonadotropin hormone release and the onset of puberty. Pssm-ID: 320669 [Multi-domain] Cd Length: 282 Bit Score: 62.64 E-value: 3.60e-11
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| 7tmA_NPY2R | cd15399 | neuropeptide Y receptor type 2, member of the class A family of seven-transmembrane G ... |
82-325 | 3.80e-11 | |||||
neuropeptide Y receptor type 2, member of the class A family of seven-transmembrane G protein-coupled receptors; NPY is a 36-amino acid peptide neurotransmitter with a C-terminal tyrosine amide residue that is widely distributed in the brain and the autonomic nervous system of many mammalian species. NPY exerts its functions through five, G-protein coupled receptor subtypes including NPY1R, NPY2R, NPY4R, NPY5R, and NPY6R; however, NPY6R is not functional in humans. NYP receptors are also activated by its two other family members, peptide YY (PYY) and pancreatic polypeptide (PP). They typically couple to G(i) or G(o) proteins, which leads to a decrease in adenylate cyclase activity, thereby decreasing intracellular cAMP levels, and are involved in diverse physiological roles including appetite regulation, circadian rhythm, and anxiety. When NPY signals through NPY2R in concert with NPY5R, it induces angiogenesis and consequently plays an important role in revascularization and wound healing. On the other hand, when NPY acts through NPY1R and NPYR5, it acts as a vascular mitogen, leading to restenosis and atherosclerosis. Pssm-ID: 320521 [Multi-domain] Cd Length: 285 Bit Score: 62.91 E-value: 3.80e-11
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| 7tmA_FPR-like | cd15117 | N-formyl peptide receptors, member of the class A family of seven-transmembrane G ... |
106-323 | 4.80e-11 | |||||
N-formyl peptide receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; The formyl peptide receptors (FPRs) are chemoattractant GPCRs that involved in mediating immune responses to infection. They are expressed at elevated levels on polymorphonuclear and mononuclear phagocytes. FPRs bind N-formyl peptides, which are derived from the mitochondrial proteins of ruptured host cells or invading pathogens. Activation of FPRs by N-formyl peptides such as N-formyl-Met-Leu-Phe (FMLP) triggers a signaling cascade that stimulates neutrophil accumulation, phagocytosis and superoxide production. These responses are mediated through a pertussis toxin-sensitive G(i) protein that activates a PLC-IP3-calcium signaling pathway. While FPRs are involved in host defense responses to bacterial infection, they can also suppress the immune system under certain conditions. Yet, the physiological role of the FPR family is not fully understood. Pssm-ID: 320245 [Multi-domain] Cd Length: 288 Bit Score: 62.44 E-value: 4.80e-11
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| 7tmA_AstA_R_insect | cd15096 | allatostatin-A receptor in insects, member of the class A family of seven-transmembrane G ... |
78-327 | 5.19e-11 | |||||
allatostatin-A receptor in insects, member of the class A family of seven-transmembrane G protein-coupled receptors; The G protein-coupled AstA receptor binds allatostatin A. Three distinct types of allatostatin have been identified in the insects and crustaceans: AstA, AstB, and AstC. They both inhibit the biosynthesis of juvenile hormone and exert an inhibitory influence on food intake. Therefore, allatostatins are considered as potential targets for insect control. Pssm-ID: 320224 [Multi-domain] Cd Length: 284 Bit Score: 62.31 E-value: 5.19e-11
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| 7tmA_Prostanoid_R | cd14981 | G protein-coupled receptors for prostanoids, member of the class A family of ... |
106-323 | 6.20e-11 | |||||
G protein-coupled receptors for prostanoids, member of the class A family of seven-transmembrane G protein-coupled receptors; Prostanoids are the cyclooxygenase (COX) metabolites of arachidonic acid, which include the prostaglandins (PGD2, PGE2, PGF2alpha), prostacyclin (PGI2), and thromboxane A2 (TxA2). These five major bioactive prostanoids acts as mediators or modulators in a wide range of physiological and pathophysiological processes within the kidney and play important roles in inflammation, platelet aggregation, and vasoconstriction/relaxation, among many others. They act locally by preferentially interacting with G protein-coupled receptors designated DP, EP. FP, IP, and TP, respectively. The phylogenetic tree suggests that the prostanoid receptors can be grouped into two major branches: G(s)-coupled (DP1, EP2, EP4, and IP) and G(i)- (EP3) or G(q)-coupled (EP1, FP, and TP), forming three clusters. Pssm-ID: 320112 [Multi-domain] Cd Length: 288 Bit Score: 62.26 E-value: 6.20e-11
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| 7tmA_GPR25 | cd15193 | G protein-coupled receptor 25, member of the class A family of seven-transmembrane G ... |
37-323 | 6.29e-11 | |||||
G protein-coupled receptor 25, member of the class A family of seven-transmembrane G protein-coupled receptors; GPR25 is an orphan G-protein coupled receptor that shares strong sequence homology to GPR15 and the angiotensin II receptors. These closely related receptors form a group within the class A G-protein coupled receptors (GPCRs). GPR15 controls homing of T cells, especially FOXP3(+) regulatory T cells, to the large intestine mucosa and thereby mediates local immune homeostasis. Moreover, GRP15-deficient mice were shown to be prone to develop more severe large intestine inflammation. Angiotensin II (Ang II), the main effector in the renin-angiotensin system, plays a crucial role in the regulation of cardiovascular homeostasis through its type 1 (AT1) and type 2 (AT2) receptors. Pssm-ID: 320321 [Multi-domain] Cd Length: 279 Bit Score: 62.08 E-value: 6.29e-11
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| 7tmA_GHSR-like | cd15928 | growth hormone secretagogue receptor, motilin receptor, and related proteins, member of the ... |
78-327 | 8.59e-11 | |||||
growth hormone secretagogue receptor, motilin receptor, and related proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This subfamily includes growth hormone secretagogue receptor (GHSR or ghrelin receptor), motilin receptor (also called GPR38), and related proteins. Both GHSR and GPR38 bind peptide hormones. Ghrelin, the endogenous ligand for GHSR, is an acylated 28-amino acid peptide hormone produced by ghrelin cells in the gastrointestinal tract. Ghrelin is also called the hunger hormone and is involved in the regulation of growth hormone release, appetite and feeding, gut motility, lipid and glucose metabolism, and energy balance. Motilin, the ligand for GPR38, is a 22 amino acid peptide hormone expressed throughout the gastrointestinal tract and stimulates contraction of gut smooth muscle. It is involved in the regulation of digestive tract motility. Pssm-ID: 320594 [Multi-domain] Cd Length: 288 Bit Score: 61.74 E-value: 8.59e-11
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| 7tmA_GPR65_TDAG8 | cd15365 | proton-sensing G protein-coupled receptor 65, member of the class A family of ... |
71-327 | 8.82e-11 | |||||
proton-sensing G protein-coupled receptor 65, member of the class A family of seven-transmembrane G protein-coupled receptors; The T cell death associated gene-8 receptor (TDAG8, also known as GPR65) is a member of the proton-sensing G-protein-coupled receptor (GPCR) family which also includes the G2 accumulation receptor (G2A, also known as GPR132), ovarian cancer G-protein receptor 1 (OGR-1, GPR68), and G-protein-coupled receptor 4 (GPR4). Proton-sensing G-protein coupled receptors sense pH of 7.6 to 6.0 and mediates a variety of biological activities in neutral and mildly acidic pH conditions, whereas the acid-sensing ionotropic ion channels typically sense strong acidic pH. Activation of TDAG8 by extracellular acidosis increases the cAMP production, stimulates Rho, and induces stress fiber formation. TDAG8 has also been shown to regulate the extracellular acidosis-induced inhibition of pro-inflammatory cytokine production in peritoneal macrophages. Pssm-ID: 320487 [Multi-domain] Cd Length: 277 Bit Score: 61.72 E-value: 8.82e-11
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| 7tmA_AT2R | cd15191 | type 2 angiotensin II receptor, member of the class A family of seven-transmembrane G ... |
107-323 | 1.01e-10 | |||||
type 2 angiotensin II receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; Angiotensin II (Ang II), the main effector in the renin-angiotensin system, plays a crucial role in the regulation of cardiovascular homeostasis through its type 1 (AT1) and type 2 (AT2) receptors. Ang II contributes to cardiovascular diseases such as hypertension and atherosclerosis via AT1R activation. Ang II increases blood pressure through Gq-mediated activation of phospholipase C, resulting in phosphoinositide (PI) hydrolysis and increased intracellular calcium levels. Through the AT2R, Ang II counteracts the vasoconstrictor action of AT1R and thereby induces vasodilation, sodium excretion, and reduction of blood pressure. Moreover, AT1R promotes cell proliferation, whereas AT2R inhibits proliferation and stimulates cell differentiation. The AT2R is highly expressed during fetal development, however it is scarcely present in adult tissues and is induced in pathological conditions. Generally, the AT1R mediates many actions of Ang II, while the AT2R is involved in the regulation of blood pressure and renal function. Pssm-ID: 341341 [Multi-domain] Cd Length: 285 Bit Score: 61.30 E-value: 1.01e-10
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| 7tmA_NK1R | cd16002 | neurokinin 1 receptor, member of the class A family of seven-transmembrane G protein-coupled ... |
106-323 | 1.05e-10 | |||||
neurokinin 1 receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; The neurokinin 1 receptor (NK1R), also known as tachykinin receptor 1 (TACR1) or substance P receptor (SPR), is a G-protein coupled receptor found in the mammalian central nervous and peripheral nervous systems. The tachykinins act as excitatory transmitters on neurons and cells in the gastrointestinal tract. The TKs are characterized by a common five-amino acid C-terminal sequence, Phe-X-Gly-Leu-Met-NH2, where X is a hydrophobic residue. The three major mammalian tachykinins are substance P (SP), neurokinin A (NKA), and neurokinin B (NKB). The physiological actions of tachykinins are mediated through three types of receptors: neurokinin receptor type 1 (NK1R), NK2R, and NK3R. SP is a high-affinity endogenous ligand for NK1R, which interacts with the Gq protein and activates phospholipase C, leading to elevation of intracellular calcium. SP is an extremely potent vasodilator through endothelium dependent mechanism and is released from the autonomic sensory nerves. NK2R is a high-affinity receptor for NKA, the tachykinin neuropeptide substance K. SP and NKA are found in the enteric nervous system and mediate in the regulation of gastrointestinal motility, secretion, vascular permeability, and pain perception. Pssm-ID: 320668 [Multi-domain] Cd Length: 284 Bit Score: 61.42 E-value: 1.05e-10
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| 7tmA_TAAR2_3_4 | cd15312 | trace amine-associated receptors 2, 3, 4, and similar receptors, member of the class A family ... |
78-326 | 1.63e-10 | |||||
trace amine-associated receptors 2, 3, 4, and similar receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; TAAR2, TAAR3, and TAAR4 are among the 15 identified trace amine-associated receptor subtypes, which form a distinct subfamily within the class A G protein-coupled receptor family. Trace amines are endogenous amines of unknown function that have strong structural and metabolic similarity to classical monoamine neurotransmitters (serotonin, noradrenaline, adrenaline, dopamine, and histamine), which play critical roles in human and animal physiological activities such as cognition, consciousness, mood, motivation, perception, and autonomic responses. However, trace amines are found in the mammalian brain at very low concentrations compared to classical monoamines. Trace amines, including p-tyramine, beta-phenylethylamine, and tryptamine, are also thought to act as chemical messengers to exert their biological effects in vertebrates. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320437 [Multi-domain] Cd Length: 289 Bit Score: 60.83 E-value: 1.63e-10
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| 7tmA_CXCR5 | cd15181 | CXC chemokine receptor type 5, member of the class A family of seven-transmembrane G ... |
45-285 | 1.68e-10 | |||||
CXC chemokine receptor type 5, member of the class A family of seven-transmembrane G protein-coupled receptors; CXCR5 is a B-cell selective receptor that binds specifically to the homeostatic chemokine CXCL13 and regulates adaptive immunity. The receptor is found on all peripheral blood and tonsillar B cells and is involved in lymphocyte migration (homing) to specific tissues and development of normal lymphoid tissue. Chemokines are principal regulators for leukocyte trafficking, recruitment, and activation. Chemokine family membership is defined on the basis of sequence homology and on the presence of variations on a conserved cysteine motif, which allows the family to further divide into four subfamilies (CC, CXC, XC, and CX3C). Chemokines interact with seven-transmembrane receptors which are typically coupled to G protein for signaling. Currently, there are ten known receptors for CC chemokines, seven for CXC chemokines, and single receptors for the XC and CX3C chemokines. Pssm-ID: 341336 [Multi-domain] Cd Length: 281 Bit Score: 60.92 E-value: 1.68e-10
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| 7tmA_5-HT4 | cd15056 | serotonin receptor subtype 4, member of the class A family of seven-transmembrane G ... |
83-326 | 2.00e-10 | |||||
serotonin receptor subtype 4, member of the class A family of seven-transmembrane G protein-coupled receptors; The 5-HT4 subtype is a member of the serotonin receptor family that belongs to the class A G protein-coupled receptors, and binds the neurotransmitter serotonin (5HT; 5-hydroxytryptamine) in the mammalian central nervous system (CNS). 5-HT4 receptors are selectively linked to G proteins of the G(s) family, which positively stimulate adenylate cyclase, causing cAMP formation and activation of protein kinase A. 5-HT4 receptor-specific agonists have been shown to enhance learning and memory in animal studies. Moreover, hippocampal 5-HT4 receptor expression has been reported to be inversely correlated with memory performance in humans. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320184 [Multi-domain] Cd Length: 294 Bit Score: 60.58 E-value: 2.00e-10
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| 7tmA_GPR17 | cd15161 | G protein-coupled receptor 17, member of the class A family of seven-transmembrane G ... |
77-323 | 2.36e-10 | |||||
G protein-coupled receptor 17, member of the class A family of seven-transmembrane G protein-coupled receptors; GPR17 is a Forkhead box protein O1 (FOXO1) target and abundantly expressed in agouti-related peptide (AGRP) neurons. FOXO1 is a transcription factor that plays key roles in regulation of gluconeogenesis and glycogenolysis by insulin signaling. For instance, food intake and body weight increase when hypothalamic FOXO1 is activated, whereas they both decrease when FOXO1 is inhibited. However, a recent study has been reported that GPR17 deficiency in mice did not affect food intake or glucose homeostasis. Thus, GPR17 may not play a role in the control of food intake, body weight, or glycemic control. GPR17 is phylogenetically closely related to purinergic P2Y and cysteinyl-leukotriene receptors. Pssm-ID: 320289 [Multi-domain] Cd Length: 277 Bit Score: 60.11 E-value: 2.36e-10
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| 7tmA_GPR1 | cd15119 | G protein-coupled receptor 1 for chemerin, member of the class A family of seven-transmembrane ... |
107-323 | 2.39e-10 | |||||
G protein-coupled receptor 1 for chemerin, member of the class A family of seven-transmembrane G protein-coupled receptors; G-protein coupled receptor 1 (GPR1) belongs to the class A of the seven transmembrane domain receptors. This is an orphan receptor that can be activated by the leukocyte chemoattractant chemerin, thereby suggesting that some of the anti-inflammatory actions of chemerin may be mediated through GPR1. GPR1 is most closely related to another chemerin receptor CMKLR1. In an in-vitro study, GPR1 has been shown to act as a co-receptor to allow replication of HIV viruses. Pssm-ID: 320247 [Multi-domain] Cd Length: 278 Bit Score: 60.14 E-value: 2.39e-10
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| 7tmA_NPR-like_invertebrate | cd15391 | invertebrate neuropeptide receptor-like, member of the class A family of seven-transmembrane G ... |
76-327 | 2.41e-10 | |||||
invertebrate neuropeptide receptor-like, member of the class A family of seven-transmembrane G protein-coupled receptors; This subgroup includes putative neuropeptide receptor found in invertebrates, which is a member of class A of 7-transmembrane G protein-coupled receptors. This orphan receptor shares a significant amino acid sequence identity with the neurokinin 1 receptor (NK1R). The endogenous ligand for NK1R is substance P, an 11-amino acid peptide that functions as a vasodilator and neurotransmitter and is released from the autonomic sensory nerve fibers. Pssm-ID: 320513 [Multi-domain] Cd Length: 289 Bit Score: 60.22 E-value: 2.41e-10
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| 7tmA_NOFQ_opioid_R | cd15092 | nociceptin/orphanin FQ peptide receptor, member of the class A family of seven-transmembrane G ... |
82-326 | 3.27e-10 | |||||
nociceptin/orphanin FQ peptide receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; The nociceptin (NOP) receptor binds nociceptin or orphanin FQ, a 17 amino acid endogenous neuropeptide. The NOP receptor is involved in the modulation of various brain activities including instinctive and emotional behaviors. The opioid receptor family is composed of four major subtypes: mu (MOP), delta (DOP), kappa (KOP) opioid receptors, and the nociceptin/orphanin FQ peptide receptor (NOP). They are distributed widely in the central nervous system and respond to classic alkaloid opiates, such as morphine and heroin, as well as to endogenous peptide ligands, which include dynorphins, enkephalins, endorphins, endomorphins, and nociceptin. Opioid receptors are coupled to inhibitory G proteins of the G(i/o) family and involved in regulating a variety of physiological functions such as pain, addiction, mood, stress, epileptic seizure, and obesity, among many others. Pssm-ID: 320220 [Multi-domain] Cd Length: 279 Bit Score: 59.88 E-value: 3.27e-10
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| 7tmA_CXCR4 | cd15179 | CXC chemokine receptor type 4, member of the class A family of seven-transmembrane G ... |
71-285 | 4.10e-10 | |||||
CXC chemokine receptor type 4, member of the class A family of seven-transmembrane G protein-coupled receptors; CXCR4 is the only known G protein-coupled chemokine receptor for the key homeostatic ligand CXCL12, which is constitutively secreted by bone marrow stromal cells. Atypical chemokine receptor CXCR7 (ACKR3) also binds CXCL12, but activates signaling in a G protein-independent manner. CXCR4 is also a co-receptor for HIV infection and plays critical roles in the development of immune system during both lymphopoiesis and myelopoiesis. Chemokines are principal regulators for leukocyte trafficking, recruitment, and activation. Chemokine family membership is defined on the basis of sequence homology and on the presence of variations on a conserved cysteine motif, which allows the family to further divide into four subfamilies (CC, CXC, XC, and CX3C). Chemokines interact with seven-transmembrane receptors which are typically coupled to G protein for signaling. Currently, there are ten known receptors for CC chemokines, seven for CXC chemokines, and single receptors for the XC and CX3C chemokines. Pssm-ID: 341334 [Multi-domain] Cd Length: 278 Bit Score: 59.78 E-value: 4.10e-10
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| 7tmA_NPY4R | cd15397 | neuropeptide Y receptor type 4, member of the class A family of seven-transmembrane G ... |
78-325 | 4.98e-10 | |||||
neuropeptide Y receptor type 4, member of the class A family of seven-transmembrane G protein-coupled receptors; NPY is a 36-amino acid peptide neurotransmitter with a C-terminal tyrosine amide residue that is widely distributed in the brain and the autonomic nervous system of many mammalian species. NPY exerts its functions through five, G-protein coupled receptor subtypes including NPY1R, NPY2R, NPY4R, NPY5R, and NPY6R; however, NPY6R is not functional in humans. NYP receptors are also activated by its two other family members, peptide YY (PYY) and pancreatic polypeptide (PP). They typically couple to G(i) or G(o) proteins, which leads to a decrease in adenylate cyclase activity, thereby decreasing intracellular cAMP levels, and are involved in diverse physiological roles including appetite regulation, circadian rhythm, and anxiety. Pssm-ID: 320519 [Multi-domain] Cd Length: 293 Bit Score: 59.37 E-value: 4.98e-10
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| 7tmA_TAAR6_8_9 | cd15316 | trace amine-associated receptors 6, 8, and 9, member of the class A family of ... |
79-326 | 5.26e-10 | |||||
trace amine-associated receptors 6, 8, and 9, member of the class A family of seven-transmembrane G protein-coupled receptors; Included in this group are mammalian TAAR6, TAAR8, TAAR9, and similar proteins. They are among the 15 identified amine-associated receptors (TAARs), a distinct subfamily within the class A G protein-coupled receptors. Trace amines are endogenous amines of unknown function that have strong structural and metabolic similarity to classical monoamine neurotransmitters (serotonin, noradrenaline, adrenaline, dopamine, and histamine), which play critical roles in human and animal physiological activities such as cognition, consciousness, mood, motivation, perception, and autonomic responses. However, trace amines are found in the mammalian brain at very low concentrations compared to classical monoamines. Trace amines, including p-tyramine, beta-phenylethylamine, and tryptamine, are also thought to act as chemical messengers to exert their biological effects in vertebrates. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320439 [Multi-domain] Cd Length: 290 Bit Score: 59.49 E-value: 5.26e-10
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| 7tmA_P2Y1-like | cd15168 | P2Y purinoceptors 1, 2, 4, 6, 11 and similar proteins, member of the class A family of ... |
107-323 | 7.69e-10 | |||||
P2Y purinoceptors 1, 2, 4, 6, 11 and similar proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; The P2Y receptor family is composed of eight subtypes, which are activated by naturally occurring extracellular nucleotides such as ATP, ADP, UTP, UDP, and UDP-glucose. These eight receptors are ubiquitous in human tissues and can be further classified into two subfamilies based on sequence homology and second messenger coupling: a subfamily of five P2Y1-like receptors (P2Y1, P2Y2, P2Y4, P2Y6, and P2Y11Rs) that are coupled to G(q) protein to activate phospholipase C (PLC) and a second subfamily of three P2Y12-like receptors (P2Y12, P2YR13, and P2Y14Rs) that are coupled to G(i) protein to inhibit adenylate cyclase. Several cloned subtypes, such as P2Y3, P2Y5, and P2Y7-10, are not functional mammalian nucleotide receptors. The native agonists for P2Y receptors are: ATP (P2Y2, P2Y12), ADP (P2Y1, P2Y12, and P2Y13), UTP (P2Y2, P2Y4), UDP (P2Y6, P2Y14), and UDP-glucose (P2Y14). This cluster only includes P2Y1-like receptors as well as other closely related orphan receptors, such as GPR91 (a succinate receptor) and GPR80/GPR99 (an alpha-ketoglutarate receptor). Pssm-ID: 341329 [Multi-domain] Cd Length: 284 Bit Score: 58.87 E-value: 7.69e-10
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| 7tmA_Beta3_AR | cd15959 | beta-3 adrenergic receptors (adrenoceptors), member of the class A family of ... |
83-323 | 8.71e-10 | |||||
beta-3 adrenergic receptors (adrenoceptors), member of the class A family of seven-transmembrane G protein-coupled receptors; The beta-3 adrenergic receptor (beta-3 adrenoceptor), also known as beta-3 AR, is activated by adrenaline and plays important roles in regulating cardiac function and heart rate. The human heart contains three subtypes of the beta AR: beta-1 AR, beta-2 AR, and beta-3 AR. Beta-1 AR and beta-2 AR, which expressed at about a ratio of 70:30, are the major subtypes involved in modulating cardiac contractility and heart rate by positively stimulating the G(s) protein-adenylate cyclase-cAMP-PKA signaling pathway. In contrast, beta-3 AR produces negative inotropic effects by activating inhibitory G(i) proteins. The aberrant expression of betrayers can lead to cardiac dysfunction such as arrhythmias or heart failure. Pssm-ID: 320625 [Multi-domain] Cd Length: 302 Bit Score: 58.77 E-value: 8.71e-10
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| 7tmA_NPFFR1 | cd15981 | neuropeptide FF receptor 1, member of the class A family of seven-transmembrane G ... |
78-327 | 9.06e-10 | |||||
neuropeptide FF receptor 1, member of the class A family of seven-transmembrane G protein-coupled receptors; Neuropeptide FF (NPFF) is a mammalian octapeptide that belongs to a family of neuropeptides containing an RF-amide motif at their C-terminus that have been implicated in a wide range of physiological functions in the brain including pain sensitivity, insulin release, food intake, memory, blood pressure, and opioid-induced tolerance and hyperalgesia. The effects of these peptides are mediated through neuropeptide FF1 and FF2 receptors (NPFF1-R and NPFF2-R) which are predominantly expressed in the brain. NPFF induces pro-nociceptive effects, mainly through the NPFF1-R, and anti-nociceptive effects, mainly through the NPFF2-R. NPFF has been shown to inhibit adenylate cyclase via the Gi protein coupled to NPFF1-R. Pssm-ID: 320647 [Multi-domain] Cd Length: 299 Bit Score: 58.68 E-value: 9.06e-10
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| 7tmA_mAChR_DM1-like | cd15301 | muscarinic acetylcholine receptor DM1, member of the class A family of seven-transmembrane G ... |
83-323 | 1.00e-09 | |||||
muscarinic acetylcholine receptor DM1, member of the class A family of seven-transmembrane G protein-coupled receptors; This subgroup includes muscarinic acetylcholine receptor DM1-like from invertebrates. Muscarinic acetylcholine receptors (mAChRs) regulate the activity of many fundamental central and peripheral functions. The mAChR family consists of 5 subtypes M1-M5, which can be further divided into two major groups according to their G-protein coupling preference. The M1, M3 and M5 receptors selectively interact with G proteins of the G(q/11) family, whereas the M2 and M4 receptors preferentially link to the G(i/o) types of G proteins. Activation of mAChRs by agonist (acetylcholine) leads to a variety of biochemical and electrophysiological responses. In general, the exact nature of these responses and the subsequent physiological effects mainly depend on the molecular and pharmacological identity of the activated receptor subtype(s). All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320428 [Multi-domain] Cd Length: 270 Bit Score: 58.30 E-value: 1.00e-09
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| 7tmA_photoreceptors_insect | cd15079 | insect photoreceptors R1-R6 and similar proteins, member of the class A family of ... |
92-324 | 1.42e-09 | |||||
insect photoreceptors R1-R6 and similar proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes the insect photoreceptors and their closely related proteins. The Drosophila eye is composed of about 800 unit eyes called ommatidia, each of which contains eight photoreceptor cells (R1-R8). The six outer photoreceptors (R1-R6) function like the vertebrate rods and are responsible for motion detection in dim light and image formation. The R1-R6 photoreceptors express a blue-absorbing pigment, Rhodopsin 1(Rh1). The inner photoreceptors (R7 and R8) are considered the equivalent of the color-sensitive vertebrate cone cells, which express a range of different pigments. The R7 photoreceptors express one of two different UV absorbing pigments, either Rh3 or Rh4. Likewise, the R8 photoreceptors express either the blue absorbing pigment Rh5 or green absorbing pigment Rh6. These photoreceptors belong the class A of the G protein-coupled receptors and possess seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. Pssm-ID: 320207 [Multi-domain] Cd Length: 292 Bit Score: 57.97 E-value: 1.42e-09
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| 7tmA_alpha2C_AR | cd15323 | alpha-2 adrenergic receptors subtype C, member of the class A family of seven-transmembrane G ... |
78-327 | 1.72e-09 | |||||
alpha-2 adrenergic receptors subtype C, member of the class A family of seven-transmembrane G protein-coupled receptors; The alpha-2 adrenergic receptors (or adrenoceptors) are a subfamily of the class A rhodopsin-like GPCRs that share a common architecture of seven transmembrane helices. This subfamily consists of three highly homologous receptor subtypes that have a key role in neurotransmitter release: alpha-2A, alpha-2B, and alpha-2C. In addition, a fourth subtype, alpha-2D is present in ray-finned fishes and amphibians, but is not found in humans. The alpha-2 receptors are found in both central and peripheral nervous system and serve to produce inhibitory functions through the G(i) proteins. Thus, the alpha-2 receptors inhibit adenylate cyclase, which decreases cAMP production and thereby decreases calcium influx during the action potential. Consequently, lowered levels of calcium will lead to a decrease in neurotransmitter release by negative feedback. Pssm-ID: 320446 [Multi-domain] Cd Length: 261 Bit Score: 57.64 E-value: 1.72e-09
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| 7tmA_Histamine_H2R | cd15051 | histamine subtype H2 receptor, member of the class A family of seven-transmembrane G ... |
83-327 | 2.05e-09 | |||||
histamine subtype H2 receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes histamine receptor subtype H2R, a member of histamine receptor family, which belongs to the class A of GPCRs. Histamine plays a key role as chemical mediator and neurotransmitter in various physiological and pathophysiological processes in the central and peripheral nervous system. Histamine exerts its functions by binding to four different G protein-coupled receptors (H1-H4). The H2R subtype selectively interacts with the G(s)-type G protein that activates adenylate cyclase, leading to increased cAMP production and activation of Protein Kinase A. H2R is found in various tissues such as the brain, stomach, and heart. Its most prominent role is in histamine-induced gastric acid secretion. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320179 [Multi-domain] Cd Length: 287 Bit Score: 57.73 E-value: 2.05e-09
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| 7tmA_GPR151 | cd15002 | G protein-coupled receptor 151, member of the class A family of seven-transmembrane G ... |
67-327 | 2.21e-09 | |||||
G protein-coupled receptor 151, member of the class A family of seven-transmembrane G protein-coupled receptors; G-protein coupled receptor 151 (GRP151) is an orphan receptor of unknown function. Its expression is conserved in habenular axonal projections of vertebrates and may be a promising novel target for psychiatric drug development. GPR151 shows high sequence similarity with galanin receptors (GALR). GPR151 is a member of the class A rhodopsin-like GPCRs, which represent a widespread protein family that includes the light-sensitive rhodopsin as well as receptors for biogenic amines, lipids, nucleotides, odorants, peptide hormones, and a variety of other ligands. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320133 [Multi-domain] Cd Length: 280 Bit Score: 57.42 E-value: 2.21e-09
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| 7tmA_GPR84-like | cd15210 | G protein-coupled receptor 84 and similar proteins, member of the class A family of ... |
69-323 | 3.02e-09 | |||||
G protein-coupled receptor 84 and similar proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; GPR84, also known as the inflammation-related G-Protein coupled receptor EX33, is a receptor for medium-chain free fatty acid (FFA) with carbon chain lengths of C9 to C14. Among these medium-chain FFAs, capric acid (C10:0), undecanoic acid (C11:0), and lauric acid (C12:0) are the most potent endogenous agonists of GPR84, whereas short-chain and long-chain saturated and unsaturated FFAs do not activate this receptor. GPR84 contains a [G/N]RY-motif instead of the highly conserved Asp-Arg-Tyr (DRY) motif found in the third transmembrane helix (TM3) of the rhodopsin-like class A receptors and important for efficient G protein-coupled signal transduction. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, which then activate the heterotrimeric G proteins. In the case of GPR84, activation of the receptor couples to a pertussis toxin sensitive G(i/o)-protein pathway. GPR84 knockout mice showed increased Th2 cytokine production including IL-4, IL-5, and IL-13 compared to wild-type mice. It has been also shown that activation of GPR84 augments lipopolysaccharide-stimulated IL-8 production in polymorphonuclear leukocytes and TNF-alpha production in macrophages, suggesting that GPR84 may function as a proinflammatory receptor. Pssm-ID: 320338 [Multi-domain] Cd Length: 254 Bit Score: 56.89 E-value: 3.02e-09
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| 7tmA_EBI2 | cd15159 | Epstein-Barr virus (EBV)-induced gene 2, member of the class A family of seven-transmembrane G ... |
69-323 | 3.11e-09 | |||||
Epstein-Barr virus (EBV)-induced gene 2, member of the class A family of seven-transmembrane G protein-coupled receptors; Epstein-Barr virus-induced G-protein coupled receptor 2 (EBI2), also called GPR183, is activated by 7alpha, 25-dihydroxyxcholesterol (7alpha, 25-OHC), an oxysterol. EBI2 was originally identified as one of major genes induced in the Burkitt's lymphoma cell line BL41by EBV infection. EBI2 is involved in regulating B cell migration and responses, and is also implicated in human diseases such as type I diabetes, multiple sclerosis, and cancers. Pssm-ID: 320287 [Multi-domain] Cd Length: 286 Bit Score: 56.98 E-value: 3.11e-09
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| 7tmA_NTSR1 | cd15355 | neurotensin receptor subtype 1, member of the class A family of seven-transmembrane G ... |
80-327 | 3.41e-09 | |||||
neurotensin receptor subtype 1, member of the class A family of seven-transmembrane G protein-coupled receptors; Neurotensin (NTS) is a 13 amino-acid neuropeptide that functions as both a neurotransmitter and a hormone in the nervous system and peripheral tissues, respectively. NTS exerts various biological activities through activation of the G protein-coupled neurotensin receptors, NTSR1 and NTSR2. In the brain, NTS is involved in the modulation of dopamine neurotransmission, opioid-independent analgesia, hypothermia, and the inhibition of food intake, while in the periphery NTS promotes the growth of various normal and cancer cells and acts as a paracrine and endocrine modulator of the digestive tract. The third neurotensin receptor, NTSR3 or also called sortilin, is not a G protein-coupled receptor. Pssm-ID: 320477 [Multi-domain] Cd Length: 310 Bit Score: 57.16 E-value: 3.41e-09
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| 7tmA_CysLTR1 | cd15158 | cysteinyl leukotriene receptor 1, member of the class A family of seven-transmembrane G ... |
106-327 | 3.66e-09 | |||||
cysteinyl leukotriene receptor 1, member of the class A family of seven-transmembrane G protein-coupled receptors; Cysteinyl leukotrienes (LTC4, LTD4, and LTE4) are the most potent inflammatory lipid mediators that play an important role in human asthma. They are synthesized in the leucocytes (cells of immune system) from arachidonic acid by the actions of 5-lipoxygenase and induce bronchial constriction through G protein-coupled receptors, CysLTR1 and CysLTR2. Activation of CysLTR1 by LTD4 induces airway smooth muscle contraction and proliferation, eosinophil migration, and damage to the lung tissue. They belong to the class A GPCR superfamily, which all have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320286 [Multi-domain] Cd Length: 285 Bit Score: 56.68 E-value: 3.66e-09
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| 7tmA_MCHR2 | cd15339 | melanin concentrating hormone receptor 2, member of the class A family of seven-transmembrane ... |
82-288 | 3.85e-09 | |||||
melanin concentrating hormone receptor 2, member of the class A family of seven-transmembrane G protein-coupled receptors; Melanin-concentrating hormone receptor (MCHR) binds melanin concentrating hormone and is presumably involved in the neuronal regulation of food intake and energy homeostasis. Despite strong homology with somatostatin receptors, MCHR does not appear to bind somatostatin. Two MCHRs have been characterized in vertebrates, MCHR1 and MCHR2. MCHR1 is expressed in all mammals, whereas MCHR2 is only expressed in the higher order mammals, such as humans, primates, and dogs, and is not found in rodents. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320461 [Multi-domain] Cd Length: 283 Bit Score: 56.75 E-value: 3.85e-09
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| 7tmA_PSP24-like | cd15213 | G protein-coupled receptor PSP24 and similar proteins, member of the class A family of ... |
74-323 | 3.99e-09 | |||||
G protein-coupled receptor PSP24 and similar proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes two human orphan receptors, GPR45 and GPR65, and their closely related proteins found in vertebrates and invertebrates. GPR45 and GPR 65 are also called PSP24-alpha (or PSP24-1) and PSP24-beta (or PSP24-2) in other vertebrates, respectively. These receptors exhibit the highest sequence homology to each other. PSP24 was originally identified as a novel, high-affinity lysophosphatidic acid (LPA) receptor in Xenopus laevis oocytes; however, PSP24 receptors (GPR45 and GPR63) have not been shown to be activated by LPA. Instead, sphingosine 1-phosphate and dioleoylphosphatidic acid have been shown to act as low affinity agonists for GPR63. PSP24 receptors are highly expressed in neuronal cells of cerebellum and their expression level remains constant from the early embryonic stages to adulthood, suggesting the important role of PSP24s in brain neuronal functions. Members of this subgroup contain the highly conserved Asp-Arg-Tyr/Phe (DRY/F) motif found in the third transmembrane helix (TM3) of the rhodopsin-like class A receptors which is important for efficient G protein-coupled signal transduction. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320341 [Multi-domain] Cd Length: 262 Bit Score: 56.60 E-value: 3.99e-09
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| 7tmA_PAR1 | cd15369 | protease-activated receptor 1, member of the class A family of seven-transmembrane G ... |
45-327 | 4.19e-09 | |||||
protease-activated receptor 1, member of the class A family of seven-transmembrane G protein-coupled receptors; Protease-acted receptors (PARs) are seven-transmembrane proteins that belong to the class A G-protein coupled receptor (GPCR) family. Four different types of the protease-activated receptors have been identified: PAR1, PAR2, PAR3, and PAR4. PARs are predominantly expressed in platelets and are activated by serine proteases such as thrombin, trypsin, and tryptase. These proteases cleave the extracellular domain of the receptor to form a new N-terminus, which in turn functions as a tethered ligand. The newly-formed tethered ligand binds intramolecularly to activate the receptor and triggers G-protein binding and intracellular signaling. PAR1, PA3, and PAR4 are activated by thrombin, whereas PAR2 is activated by trypsin. The PARs are known to couple with several G-proteins including Gi (cAMP inhibitory), G12/13 (Rho and Ras activation), and Gq (calcium signaling) to activate downstream signaling messengers which induces numerous cellular and physiological effects. Pssm-ID: 320491 Cd Length: 281 Bit Score: 56.70 E-value: 4.19e-09
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| 7tmA_PAR3 | cd15371 | protease-activated receptor 3, member of the class A family of seven-transmembrane G ... |
107-327 | 4.21e-09 | |||||
protease-activated receptor 3, member of the class A family of seven-transmembrane G protein-coupled receptors; Protease-acted receptors (PARs) are seven-transmembrane proteins that belong to the class A G-protein coupled receptor (GPCR) family. Four different types of the protease-activated receptors have been identified: PAR1, PAR2, PAR3, and PAR4. PARs are predominantly expressed in platelets and are activated by serine proteases such as thrombin, trypsin, and tryptase. These proteases cleave the extracellular domain of the receptor to form a new N-terminus, which in turn functions as a tethered ligand. The newly-formed tethered ligand binds intramolecularly to activate the receptor and triggers G-protein binding and intracellular signaling. PAR1, PA3, and PAR4 are activated by thrombin, whereas PAR2 is activated by trypsin. The PARs are known to couple with several G-proteins including Gi (cAMP inhibitory), G12/13 (Rho and Ras activation), and Gq (calcium signaling) to activate downstream signaling messengers which induces numerous cellular and physiological effects. Pssm-ID: 320493 [Multi-domain] Cd Length: 274 Bit Score: 56.73 E-value: 4.21e-09
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| 7tmA_Opsin5_neuropsin | cd15074 | neuropsin (Opsin-5), member of the class A family of seven-transmembrane G protein-coupled ... |
44-289 | 5.79e-09 | |||||
neuropsin (Opsin-5), member of the class A family of seven-transmembrane G protein-coupled receptors; Neuropsin, also known as Opsin-5, is a photoreceptor protein expressed in the retina, brain, testes, and spinal cord. Neuropsin belongs to the type 2 opsin family of the class A G-protein coupled receptors. Mammalian neuropsin activates Gi protein-mediated photo-transduction pathway in a UV-dependent manner, whereas, in non-mammalian vertebrates, neuropsin is involved in regulating the photoperiodic control of seasonal reproduction in birds such as quail. As with other opsins, it may also act as a retinal photoisomerase. Pssm-ID: 320202 [Multi-domain] Cd Length: 284 Bit Score: 56.13 E-value: 5.79e-09
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| 7tmA_5-HT1A_vertebrates | cd15330 | serotonin receptor subtype 1A from vertebrates, member of the class A family of ... |
79-327 | 6.15e-09 | |||||
serotonin receptor subtype 1A from vertebrates, member of the class A family of seven-transmembrane G protein-coupled receptors; The 5-HT1 receptors, one of 14 mammalian 5-HT receptors, is a member of the class A of GPCRs and is activated by the endogenous neurotransmitter and peripheral signal mediator serotonin (5-hydroxytryptamine, 5-HT). The 5-HT1 receptors mediate inhibitory neurotransmission by coupling to G proteins of the G(i/o) family, which lead to a decrease in adenylate cyclase activity, thereby decreasing intracellular cAMP levels and calcium influx. The 5-HT1 receptor subfamily includes 5 subtypes: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F. There is no 5-HT1C receptor subtype, as it has been reclassified as the 5-HT2C receptor. In the CNS, serotonin is involved in the regulation of appetite, mood, sleep, cognition, learning and memory, as well as implicated in neurologic disorders such as migraine, schizophrenia, and depression. Pssm-ID: 320453 [Multi-domain] Cd Length: 260 Bit Score: 55.76 E-value: 6.15e-09
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| 7tmA_P2Y1-like | cd15967 | P2Y purinoceptor 1-like; P2Y1-like is an uncharacterized group that is phylogenetically ... |
71-286 | 6.87e-09 | |||||
P2Y purinoceptor 1-like; P2Y1-like is an uncharacterized group that is phylogenetically related to a family of purinergic G protein-coupled receptors. The P2Y receptor family is composed of eight subtypes, which are activated by naturally occurring extracellular nucleotides such as ATP, ADP, UTP, UDP, and UDP-glucose. These eight receptors are ubiquitous in human tissues and can be further classified into two subfamilies based on sequence homology and second messenger coupling: a subfamily of five P2Y1-like receptors (P2Y1, P2Y2, P2Y4, P2Y6, and P2Y11Rs) that are coupled to G(q) protein to activate phospholipase C (PLC) and a second subfamily of three P2Y12-like receptors (P2Y12, P2YR13, and P2Y14Rs) that are coupled to G(i) protein to inhibit adenylate cyclase. Several cloned subtypes, such as P2Y3, P2Y5, and P2Y7-10, are not functional mammalian nucleotide receptors. The native agonists for P2Y receptors are: ATP (P2Y2, P2Y12), ADP (P2Y1, P2Y12, and P2Y13), UTP (P2Y2, P2Y4), UDP (P2Y6, P2Y14), and UDP-glucose (P2Y14). Pssm-ID: 320633 [Multi-domain] Cd Length: 281 Bit Score: 55.85 E-value: 6.87e-09
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| 7tmA_Histamine_H1R | cd15050 | histamine subtype H1 receptor, member of the class A family of seven-transmembrane G ... |
83-323 | 7.45e-09 | |||||
histamine subtype H1 receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes histamine receptor subtype H1R, a member of histamine receptor family, which belongs to the class A of GPCRs. Histamine plays a key role as chemical mediator and neurotransmitter in various physiological and pathophysiological processes in the central and peripheral nervous system. Histamine exerts its functions by binding to four different G protein-coupled receptors (H1-H4). H1R selectively interacts with the G(q)-type G protein that activates phospholipase C and the phosphatidylinositol pathway. Antihistamines, a widely used anti-allergy medication, act on the H1 subtype and produce drowsiness as a side effect. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320178 [Multi-domain] Cd Length: 263 Bit Score: 55.51 E-value: 7.45e-09
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| 7tmA_alpha2B_AR | cd15321 | alpha-2 adrenergic receptors subtype B, member of the class A family of seven-transmembrane G ... |
78-327 | 8.26e-09 | |||||
alpha-2 adrenergic receptors subtype B, member of the class A family of seven-transmembrane G protein-coupled receptors; The alpha-2 adrenergic receptors (or adrenoceptors) are a subfamily of the class A rhodopsin-like GPCRs that share a common architecture of seven transmembrane helices. This subfamily consists of three highly homologous receptor subtypes that have a key role in neurotransmitter release: alpha-2A, alpha-2B, and alpha-2C. In addition, a fourth subtype, alpha-2D is present in ray-finned fishes and amphibians, but is not found in humans. The alpha-2 receptors are found in both central and peripheral nervous system and serve to produce inhibitory functions through the G(i) proteins. Thus, the alpha-2 receptors inhibit adenylate cyclase, which decreases cAMP production and thereby decreases calcium influx during the action potential. Consequently, lowered levels of calcium will lead to a decrease in neurotransmitter release by negative feedback. Pssm-ID: 320444 [Multi-domain] Cd Length: 268 Bit Score: 55.70 E-value: 8.26e-09
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| 7tmA_SSTR1 | cd15970 | somatostatin receptor type 1, member of the class A family of seven-transmembrane G ... |
106-327 | 8.89e-09 | |||||
somatostatin receptor type 1, member of the class A family of seven-transmembrane G protein-coupled receptors; G protein-coupled somatostatin receptors (SSTRs) are composed of five distinct subtypes (SSTR1-5) that display strong sequence similarity with opioid receptors. All five receptor subtypes bind the natural somatostatin (somatotropin release inhibiting factor), a polypeptide hormone that regulates a wide variety of physiological functions such as neurotransmission, cell proliferation, contractility of smooth muscle cells, and endocrine signaling as well as inhibition of the release of many secondary hormones. SSTR1 is coupled to a Na/H exchanger, voltage-dependent calcium channels, and AMPA/kainate glutamate channels. SSTR1 is expressed in the normal human pituitary and in nearly half of all pituitary adenoma subtypes. Pssm-ID: 320636 [Multi-domain] Cd Length: 276 Bit Score: 55.69 E-value: 8.89e-09
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| 7tmA_LPAR4 | cd15155 | lysophosphatidic acid receptor 4, member of the class A family of seven-transmembrane G ... |
69-328 | 9.50e-09 | |||||
lysophosphatidic acid receptor 4, member of the class A family of seven-transmembrane G protein-coupled receptors; Lysophosphatidic acid receptor 4 (LPAR4) is a G protein-coupled receptor that binds and is activated by the bioactive lipid lysophosphatidic acid (LPA), which is released by activated platelets and constitutively found in serum. Phylogenetic analysis of the class A GPCRs shows that LAPR4 is classified into the cluster consisting receptors that are preferentially activated by adenosine and uridine nucleotides. Although LPA6 (P2Y5) is expressed in human hair follicle cells, LPA4 and LPA5 are not. These three receptors are highly homologous and mediate an increase in intracellular cAMP production. Activation of LPAR5 is coupled to G(12/13) proteins, leading to neurite retraction and stress fiber formation, whereas coupling to G(q) protein leads to increases in calcium levels. Pssm-ID: 320283 [Multi-domain] Cd Length: 283 Bit Score: 55.70 E-value: 9.50e-09
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| 7tmA_PAFR | cd15147 | platelet-activating factor receptor, member of the class A family of seven-transmembrane G ... |
71-323 | 9.69e-09 | |||||
platelet-activating factor receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; The platelet-activating factor receptor is a G(q/11)-protein coupled receptor, which is linked to p38 MAPK and PI3K signaling pathways. PAF is a phospholipid (1-0-alkyl-2-acetyl-sn-glycero-3-phosphorylcholine) which is synthesized by cells especially involved in host defense such as platelets, macrophages, neutrophils, and monocytes. PAF is well-known for its ability to induce platelet aggregation and anaphylaxis, and also plays important roles in allergy, asthma, and inflammatory responses, among many others. Pssm-ID: 320275 [Multi-domain] Cd Length: 291 Bit Score: 55.53 E-value: 9.69e-09
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| 7tmA_P2Y12-like | cd15924 | P2Y purinoceptors 12, 13, 14, and similar proteins, member of the class A family of ... |
107-323 | 9.88e-09 | |||||
P2Y purinoceptors 12, 13, 14, and similar proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; The P2Y receptor family is composed of eight subtypes, which are activated by naturally occurring extracellular nucleotides such as ATP, ADP, UTP, UDP, and UDP-glucose. These eight receptors are ubiquitous in human tissues and can be further classified into two subfamilies based on sequence homology and second messenger coupling: a subfamily of five P2Y1-like receptors (P2Y1, P2Y2, P2Y4, P2Y6, and P2Y11Rs) that are coupled to G(q) protein to activate phospholipase C (PLC) and a second subfamily of three P2Y12-like receptors (P2Y12, P2YR13, and P2Y14Rs) that are coupled to G(i) protein to inhibit adenylate cyclase. Several cloned subtypes, such as P2Y3, P2Y5 and P2Y7-10, are not functional mammalian nucleotide receptors. The native agonists for P2Y receptors are: ATP (P2Y2, P2Y12), ADP (P2Y1, P2Y12 and P2Y13), UTP (P2Y2, P2Y4), UDP (P2Y6, P2Y14), and UDP-glucose (P2Y14). This cluster only includes P2Y12-like receptors as well as closely related orphan receptor, GPR87. Pssm-ID: 341352 [Multi-domain] Cd Length: 284 Bit Score: 55.53 E-value: 9.88e-09
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| 7tmA_Peropsin | cd15073 | retinal pigment epithelium-derived rhodopsin homolog, member of the class A family of ... |
78-323 | 1.05e-08 | |||||
retinal pigment epithelium-derived rhodopsin homolog, member of the class A family of seven-transmembrane G protein-coupled receptors; Peropsin, also known as a retinal pigment epithelium-derived rhodopsin homolog (RRH), is a visual pigment-like protein found exclusively in the apical microvilli of the retinal pigment epithelium. Peropsin belongs to the type 2 opsin family of the class A G-protein coupled receptors. Peropsin presumably plays a physiological role in the retinal pigment epithelium either by detecting light directly or monitoring the levels of retinoids, the primary light absorber in visual perception, or other pigment-related compounds in the eye. Pssm-ID: 320201 [Multi-domain] Cd Length: 280 Bit Score: 55.51 E-value: 1.05e-08
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| 7tmA_GPR101 | cd15215 | orphan G protein-coupled receptor 101, member of the class A family of seven-transmembrane G ... |
37-325 | 1.34e-08 | |||||
orphan G protein-coupled receptor 101, member of the class A family of seven-transmembrane G protein-coupled receptors; Gpr101, an orphan GPCR, is predominantly expressed in the brain within discrete nuclei and is predicted to couple to the stimulatory G(s) protein, a potent activator of adenylate cyclase. GPR101 has been implicated in mediating the actions of GnRH-(1-5), a pentapeptide formed by metallopeptidase cleavage of the decapeptide gonadotropin-releasing hormone (GnRH), which plays a critical role in the regulation of the hypothalamic-pituitary-gonadal axis. GnRH-(1-5) acts on GPR101 to stimulate epidermal growth factor (EFG) release and EFG-receptor (EGFR) phosphorylation, leading to enhanced cell migration and invasion in the Ishikawa endometrial cancer cell line. Furthermore, these effects of GnRH-(1-5) are also dependent on enzymatic activation of matrix metallopeptidase-9 (MMP-9). GPR101 is a member of the class A family of GPCRs, which includes receptors for hormones, neurotransmitters, sensory stimuli, and a variety of other ligands. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320343 [Multi-domain] Cd Length: 261 Bit Score: 54.85 E-value: 1.34e-08
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| 7tmA_CCK-AR | cd15978 | cholecystokinin receptor type A, member of the class A family of seven-transmembrane G ... |
78-323 | 1.42e-08 | |||||
cholecystokinin receptor type A, member of the class A family of seven-transmembrane G protein-coupled receptors; Cholecystokinin receptors (CCK-AR and CCK-BR) are a group of G-protein coupled receptors which bind the peptide hormones cholecystokinin (CCK) or gastrin. CCK, which facilitates digestion in the small intestine, and gastrin, a major regulator of gastric acid secretion, are highly similar peptides. Like gastrin, CCK is a naturally-occurring linear peptide that is synthesized as a preprohormone, then proteolytically cleaved to form a family of peptides with the common C-terminal sequence (Gly-Trp-Met-Asp-Phe-NH2), which is required for full biological activity. CCK-AR (type A, alimentary; also known as CCK1R) is found abundantly on pancreatic acinar cells and binds only sulfated CCK-peptides with very high affinity, whereas CCK-BR (type B, brain; also known as CCK2R), the predominant form in the brain and stomach, binds CCK or gastrin and discriminates poorly between sulfated and non-sulfated peptides. CCK is implicated in regulation of digestion, appetite control, and body weight, and is involved in neurogenesis via CCK-AR. There is some evidence to support that CCK and gastrin, via their receptors, are involved in promoting cancer development and progression, acting as growth and invasion factors. Pssm-ID: 320644 [Multi-domain] Cd Length: 278 Bit Score: 54.88 E-value: 1.42e-08
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| 7tmA_5-HT1B_1D | cd15333 | serotonin receptor subtypes 1B and 1D, member of the class A family of seven-transmembrane G ... |
33-326 | 1.47e-08 | |||||
serotonin receptor subtypes 1B and 1D, member of the class A family of seven-transmembrane G protein-coupled receptors; The 5-HT1 receptors, one of 14 mammalian 5-HT receptors, is a member of the class A of GPCRs and is activated by the endogenous neurotransmitter and peripheral signal mediator serotonin (5-hydroxytryptamine, 5-HT). The 5-HT1 receptors mediate inhibitory neurotransmission by coupling to G proteins of the G(i/o) family, which lead to a decrease in adenylate cyclase activity, thereby decreasing intracellular cAMP levels and calcium influx. The 5-HT1 receptor subfamily includes 5 subtypes: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F. There is no 5-HT1C receptor subtype, as it has been reclassified as the 5-HT2C receptor. In the CNS, serotonin is involved in the regulation of appetite, mood, sleep, cognition, learning and memory, as well as implicated in neurologic disorders such as migraine, schizophrenia, and depression. Pssm-ID: 320455 [Multi-domain] Cd Length: 265 Bit Score: 54.80 E-value: 1.47e-08
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| 7tmA_NPY1R | cd15395 | neuropeptide Y receptor type 1, member of the class A family of seven-transmembrane G ... |
78-327 | 1.54e-08 | |||||
neuropeptide Y receptor type 1, member of the class A family of seven-transmembrane G protein-coupled receptors; NPY is a 36-amino acid peptide neurotransmitter with a C-terminal tyrosine amide residue that is widely distributed in the brain and the autonomic nervous system of many mammalian species. NPY exerts its functions through five, G-protein coupled receptor subtypes including NPY1R, NPY2R, NPY4R, NPY5R, and NPY6R; however, NPY6R is not functional in humans. NYP receptors are also activated by its two other family members, peptide YY (PYY) and pancreatic polypeptide (PP). They typically couple to G(i) or G(o) proteins, which leads to a decrease in adenylate cyclase activity, thereby decreasing intracellular cAMP levels, and are involved in diverse physiological roles including appetite regulation, circadian rhythm, and anxiety. When NPY signals through NPY2R in concert with NPY5R, it induces angiogenesis and consequently plays an important role in revascularization and wound healing. On the other hand, when NPY acts through NPY1R and NPYR5, it acts as a vascular mitogen, leading to restenosis and atherosclerosis. Pssm-ID: 320517 [Multi-domain] Cd Length: 293 Bit Score: 54.82 E-value: 1.54e-08
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| 7tmA_SSTR3 | cd15972 | somatostatin receptor type 3, member of the class A family of seven-transmembrane G ... |
95-327 | 2.35e-08 | |||||
somatostatin receptor type 3, member of the class A family of seven-transmembrane G protein-coupled receptors; G protein-coupled somatostatin receptors (SSTRs) are composed of five distinct subtypes (SSTR1-5) that display strong sequence similarity with opioid receptors. All five receptor subtypes bind the natural somatostatin (somatotropin release inhibiting factor), a polypeptide hormone that regulates a wide variety of physiological functions such as neurotransmission, cell proliferation, contractility of smooth muscle cells, and endocrine signaling as well as inhibition of the release of many secondary hormones. SSTR3 is coupled to inward rectifying potassium channels. SSTR3 plays critical roles in growth hormone secretion, endothelial cell cycle arrest and apoptosis. Furthermore, SSTR3 is expressed in the normal human pituitary and in nearly half of pituitary growth hormone adenomas. Pssm-ID: 320638 [Multi-domain] Cd Length: 279 Bit Score: 54.42 E-value: 2.35e-08
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| 7tmA_5-HT1F | cd15334 | serotonin receptor subtype 1F, member of the class A family of seven-transmembrane G ... |
37-327 | 2.39e-08 | |||||
serotonin receptor subtype 1F, member of the class A family of seven-transmembrane G protein-coupled receptors; The 5-HT1 receptors, one of 14 mammalian 5-HT receptors, is a member of the class A of GPCRs and is activated by the endogenous neurotransmitter and peripheral signal mediator serotonin (5-hydroxytryptamine, 5-HT). The 5-HT1 receptors mediate inhibitory neurotransmission by coupling to G proteins of the G(i/o) family, which lead to a decrease in adenylate cyclase activity, thereby decreasing intracellular cAMP levels and calcium influx. The 5-HT1 receptor subfamily includes 5 subtypes: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F. There is no 5-HT1C receptor subtype, as it has been reclassified as the 5-HT2C receptor. In the CNS, serotonin is involved in the regulation of appetite, mood, sleep, cognition, learning and memory, as well as implicated in neurologic disorders such as migraine, schizophrenia, and depression. Pssm-ID: 320456 [Multi-domain] Cd Length: 259 Bit Score: 54.18 E-value: 2.39e-08
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| 7tmA_PAR4 | cd15372 | protease-activated receptor 4, member of the class A family of seven-transmembrane G ... |
78-327 | 2.54e-08 | |||||
protease-activated receptor 4, member of the class A family of seven-transmembrane G protein-coupled receptors; Protease-acted receptors (PARs) are seven-transmembrane proteins that belong to the class A G-protein coupled receptor (GPCR) family. Four different types of the protease-activated receptors have been identified: PAR1, PAR2, PAR3, and PAR4. PARs are predominantly expressed in platelets and are activated by serine proteases such as thrombin, trypsin, and tryptase. These proteases cleave the extracellular domain of the receptor to form a new N-terminus, which in turn functions as a tethered ligand. The newly-formed tethered ligand binds intramolecularly to activate the receptor and triggers G-protein binding and intracellular signaling. PAR1, PA3, and PAR4 are activated by thrombin, whereas PAR2 is activated by trypsin. The PARs are known to couple with several G-proteins including Gi (cAMP inhibitory), G12/13 (Rho and Ras activation), and Gq (calcium signaling) to activate downstream signaling messengers which induces numerous cellular and physiological effects. Pssm-ID: 320494 [Multi-domain] Cd Length: 274 Bit Score: 54.37 E-value: 2.54e-08
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| 7tmA_P2Y10 | cd15153 | P2Y purinoceptor 10, member of the class A family of seven-transmembrane G protein-coupled ... |
72-326 | 2.91e-08 | |||||
P2Y purinoceptor 10, member of the class A family of seven-transmembrane G protein-coupled receptors; P2Y10 receptor is a G-protein coupled receptor that is activated by both sphingosine-1-phosphate (S1P) and lysophosphatidic acid (LPA). Phylogenetic analysis of the class A GPCRs shows that P2Y10 is grouped into the cluster comprising nucleotide and lipid receptors. Although the mouse P2Y10 was found to be expressed in brain, lung, reproductive organs, and skeletal muscle, the physiological function of this receptor is not yet known. S1P and LPA are bioactive lipid molecules that induce a variety of cellular responses through G proteins: adhesion, invasion, cell migration and proliferation, among many others. Pssm-ID: 320281 [Multi-domain] Cd Length: 283 Bit Score: 54.03 E-value: 2.91e-08
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| 7tmA_Mel1C | cd15401 | melatonin receptor subtype 1C, member of the class A family of seven-transmembrane G ... |
83-324 | 2.95e-08 | |||||
melatonin receptor subtype 1C, member of the class A family of seven-transmembrane G protein-coupled receptors; Melatonin (N-acetyl-5-methoxytryptamine) is a naturally occurring sleep-promoting chemical found in vertebrates, invertebrates, bacteria, fungi, and plants. In mammals, melatonin is secreted by the pineal gland and is involved in regulation of circadian rhythms. Its production peaks during the nighttime, and is suppressed by light. Melatonin is shown to be synthesized in other organs and cells of many vertebrates, including the Harderian gland, leukocytes, skin, and the gastrointestinal (GI) tract, which contains several hundred times more melatonin than the pineal gland and is involved in the regulation of GI motility, inflammation, and sensation. Melatonin exerts its pleiotropic physiological effects through specific membrane receptors, named MT1A, MT1B, and MT1C, which belong to the class A rhodopsin-like G-protein coupled receptor family. MT1A and MT1B subtypes are present in mammals, whereas MT1C subtype has been found in amphibians and birds. The melatonin receptors couple to G proteins of the G(i/o) class, leading to the inhibition of adenylate cyclase. Pssm-ID: 320523 [Multi-domain] Cd Length: 279 Bit Score: 54.15 E-value: 2.95e-08
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| 7tmA_MCHR1 | cd15338 | melanin concentrating hormone receptor 1, member of the class A family of seven-transmembrane ... |
107-323 | 2.96e-08 | |||||
melanin concentrating hormone receptor 1, member of the class A family of seven-transmembrane G protein-coupled receptors; Melanin-concentrating hormone receptor (MCHR) binds melanin concentrating hormone and is presumably involved in the neuronal regulation of food intake and energy homeostasis. Despite strong homology with somatostatin receptors, MCHR does not appear to bind somatostatin. Two MCHRs have been characterized in vertebrates, MCHR1 and MCHR2. MCHR1 is expressed in all mammals, whereas MCHR2 is only expressed in the higher order mammals, such as humans, primates, and dogs, and is not found in rodents. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320460 [Multi-domain] Cd Length: 282 Bit Score: 54.05 E-value: 2.96e-08
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| 7tmA_mAChR_M3 | cd15299 | muscarinic acetylcholine receptor subtype M3, member of the class A family of ... |
21-286 | 3.11e-08 | |||||
muscarinic acetylcholine receptor subtype M3, member of the class A family of seven-transmembrane G protein-coupled receptors; Muscarinic acetylcholine receptors (mAChRs) regulate the activity of many fundamental central and peripheral functions. The mAChR family consists of 5 subtypes M1-M5, which can be further divided into two major groups according to their G-protein coupling preference. The M1, M3 and M5 receptors selectively interact with G proteins of the G(q/11) family, whereas the M2 and M4 receptors preferentially link to the G(i/o) types of G proteins. The M3 receptor is mainly located in smooth muscle, exocrine glands and vascular endothelium. It induces vomiting in the central nervous system and is a critical regulator of glucose homeostasis by modulating insulin secretion. Generally, M3 receptor causes contraction of smooth muscle resulting in vasoconstriction and increased glandular secretion. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320426 [Multi-domain] Cd Length: 274 Bit Score: 53.80 E-value: 3.11e-08
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| 7tmA_Bradykinin_R | cd15189 | bradykinin receptors, member of the class A family of seven-transmembrane G protein-coupled ... |
73-323 | 3.43e-08 | |||||
bradykinin receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; The bradykinin receptor family is a group of the seven transmembrane G-protein coupled receptors, whose endogenous ligand is the pro-inflammatory nonapeptide bradykinin that mediates various vascular and pain responses. Two major bradykinin receptor subtypes, B1 and B2, have been identified based on their pharmacological properties. The B1 receptor is rapidly induced by tissue injury and inflammation, whereas the B2 receptor is ubiquitously expressed on many tissue types. Both receptors contain three consensus sites for N-linked glycosylation in extracellular domains and couple to G(q) protein to activate phospholipase C, leading to phosphoinositide hydrolysis and intracellular calcium mobilization. They can also interact with G(i) protein to inhibit adenylate cyclase and activate the MAPK (mitogen-activated protein kinase) pathways. Pssm-ID: 320317 [Multi-domain] Cd Length: 284 Bit Score: 54.01 E-value: 3.43e-08
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| 7tmA_P2Y6_P2Y3-like | cd15968 | P2Y purinoceptors 6 and 3, and similar proteins, member of the class A family of ... |
43-323 | 3.55e-08 | |||||
P2Y purinoceptors 6 and 3, and similar proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes P2Y receptor 6 (P2Y6), P2Y3, and P2Y3-like proteins. These receptors belong to the G(i) class of a family of purinergic G-protein coupled receptors. In the CNS, P2Y6 plays a role in microglia activation and phagocytosis, and is involved in the secretion of interleukin from monocytes and macrophages in the immune system. The P2Y receptor family is composed of eight subtypes, which are activated by naturally occurring extracellular nucleotides such as ATP, ADP, UTP, UDP, and UDP-glucose. These eight receptors are ubiquitous in human tissues and can be further classified into two subfamilies based on sequence homology and second messenger coupling: a subfamily of five P2Y1-like receptors (P2Y1, P2Y2, P2Y4, P2Y6, and P2Y11Rs) that are coupled to G(q) protein to activate phospholipase C (PLC) and a second subfamily of three P2Y12-like receptors (P2Y12, P2YR13, and P2Y14Rs) that are coupled to G(i) protein to inhibit adenylate cyclase. Several cloned subtypes, such as P2Y3, P2Y5, and P2Y7-10, are not functional mammalian nucleotide receptors. The native agonists for P2Y receptors are: ATP (P2Y2, P2Y12), ADP (P2Y1, P2Y12, and P2Y13), UTP (P2Y2, P2Y4), UDP (P2Y6, P2Y14), and UDP-glucose (P2Y14). Pssm-ID: 320634 [Multi-domain] Cd Length: 285 Bit Score: 54.01 E-value: 3.55e-08
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| 7tmA_5-HT2 | cd15052 | serotonin receptor subtype 2, member of the class A family of seven-transmembrane G ... |
80-326 | 3.62e-08 | |||||
serotonin receptor subtype 2, member of the class A family of seven-transmembrane G protein-coupled receptors; The 5-HT2 receptors are a subfamily of serotonin receptors that bind the neurotransmitter serotonin (5HT; 5-hydroxytryptamine) in the central nervous system (CNS). The 5-HT2 subfamily is composed of three subtypes that mediate excitatory neurotransmission: 5-HT2A, 5-HT2B, and 5-HT2C. They are selectively linked to G proteins of the G(q/11) family and activate phospholipase C, which leads to activation of protein kinase C and calcium release. In the CNS, serotonin is involved in the regulation of appetite, mood, sleep, cognition, learning and memory, as well as implicated in diseases such as migraine, schizophrenia, and depression. Indeed, 5-HT2 receptors are attractive targets for a variety of psychoactive drugs, ranging from atypical antipsychotic drugs, antidepressants, and anxiolytics, which have an antagonistic action on 5-HT2 receptors, to hallucinogens, which act as agonists at postsynaptic 5-HT2 receptors. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320180 [Multi-domain] Cd Length: 262 Bit Score: 53.47 E-value: 3.62e-08
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| 7tmA_mAChR_M2 | cd15297 | muscarinic acetylcholine receptor subtype M2, member of the class A family of ... |
79-286 | 4.01e-08 | |||||
muscarinic acetylcholine receptor subtype M2, member of the class A family of seven-transmembrane G protein-coupled receptors; Muscarinic acetylcholine receptors (mAChRs) regulate the activity of many fundamental central and peripheral functions. The mAChR family consists of 5 subtypes M1-M5, which can be further divided into two major groups according to their G-protein coupling preference. The M1, M3 and M5 receptors selectively interact with G proteins of the G(q/11) family, whereas the M2 and M4 receptors preferentially link to the G(i/o) types of G proteins. Activation of M2 receptor causes a decrease in cAMP production, generally leading to inhibitory-type effects. This causes an outward current of potassium in the heart, resulting in a decreased heart rate. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320424 [Multi-domain] Cd Length: 262 Bit Score: 53.43 E-value: 4.01e-08
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| 7tmA_Ap5-HTB1-like | cd15065 | serotonin receptor subtypes B1 and B2 from Aplysia californica and similar proteins; member of ... |
83-326 | 4.02e-08 | |||||
serotonin receptor subtypes B1 and B2 from Aplysia californica and similar proteins; member of the class A family of seven-transmembrane G protein-coupled receptors; This subfamily includes Aplysia californica serotonin receptors Ap5-HTB1 and Ap5-HTB2, and similar proteins from bilateria including insects, mollusks, annelids, and worms. Ap5-HTB1 is one of the several different receptors for 5-hydroxytryptamine (5HT, serotonin). In Aplysia, serotonin plays important roles in a variety of behavioral and physiological processes mediated by the central nervous system. These include circadian clock, feeding, locomotor movement, cognition and memory, synaptic growth and synaptic plasticity. Both Ap5-HTB1 and Ap5-HTB2 receptors are coupled to G-proteins that stimulate phospholipase C, leading to the activation of phosphoinositide metabolism. Ap5-HTB1 is expressed in the reproductive system, whereas Ap5-HTB2 is expressed in the central nervous system. Pssm-ID: 320193 [Multi-domain] Cd Length: 300 Bit Score: 53.89 E-value: 4.02e-08
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| 7tmA_BK-1 | cd15380 | bradykinin receptor B1, member of the class A family of seven-transmembrane G protein-coupled ... |
73-323 | 4.03e-08 | |||||
bradykinin receptor B1, member of the class A family of seven-transmembrane G protein-coupled receptors; The bradykinin receptor family is a group of the seven transmembrane G-protein coupled receptors, whose endogenous ligand is the pro-inflammatory nonapeptide bradykinin that mediates various vascular and pain responses. Two major bradykinin receptor subtypes, B1 and B2, have been identified based on their pharmacological properties. The B1 receptor is rapidly induced by tissue injury and inflammation, whereas the B2 receptor is ubiquitously expressed on many tissue types. Both receptors contain three consensus sites for N-linked glycosylation in extracellular domains and couple to G(q) protein to activate phospholipase C, leading to phosphoinositide hydrolysis and intracellular calcium mobilization. They can also interact with G(i) protein to inhibit adenylate cyclase and activate the MAPK (mitogen-activated protein kinase) pathways. Pssm-ID: 320502 [Multi-domain] Cd Length: 286 Bit Score: 53.65 E-value: 4.03e-08
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| 7tmA_GPR34-like | cd15920 | P2Y-like receptor and similar proteins, member of the class A family of seven-transmembrane G ... |
71-327 | 4.06e-08 | |||||
P2Y-like receptor and similar proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; GPR34 is phylogenetically related to the P2Y family of purinergic G protein-coupled receptors. The P2Y receptor family is composed of eight subtypes, which are activated by naturally occurring extracellular nucleotides such as ATP, ADP, UTP, UDP, and UDP-glucose. GPR34 is shown to couple to G(i/o) protein and is highly expressed in microglia. Recently, lysophosphatidylserine has been identified as a ligand for GPR34. This group belongs to the class A G protein-coupled receptor superfamily, which all have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, which then activate the heterotrimeric G proteins. G-proteins regulate a variety of cellular functions including metabolic enzymes, ion channels, and transporters, among many others. Pssm-ID: 320586 [Multi-domain] Cd Length: 278 Bit Score: 53.65 E-value: 4.06e-08
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| 7tmA_mAChR_M1 | cd17790 | muscarinic acetylcholine receptor subtype M1, member of the class A family of ... |
21-286 | 4.20e-08 | |||||
muscarinic acetylcholine receptor subtype M1, member of the class A family of seven-transmembrane G protein-coupled receptors; Muscarinic acetylcholine receptors (mAChRs) regulate the activity of many fundamental central and peripheral functions. The mAChR family consists of 5 subtypes M1-M5, which can be further divided into two major groups according to their G-protein coupling preference. The M1, M3 and M5 receptors selectively interact with G proteins of the G(q/11) family, whereas the M2 and M4 receptors preferentially link to the G(i/o) types of G proteins. Activation of mAChRs by agonist (acetylcholine) leads to a variety of biochemical and electrophysiological responses. M1 is the dominant mAChR subtype involved in learning and memory. It is linked to synaptic plasticity, neuronal excitability, and neuronal differentiation during early development. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 341356 [Multi-domain] Cd Length: 262 Bit Score: 53.43 E-value: 4.20e-08
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| 7tmA_LTB4R1 | cd15121 | leukotriene B4 receptor subtype 1 (LTB4R1 or BLT1), member of the class A family of ... |
71-288 | 5.90e-08 | |||||
leukotriene B4 receptor subtype 1 (LTB4R1 or BLT1), member of the class A family of seven-transmembrane G protein-coupled receptors; Leukotriene B4 (LTB4), a metabolite of arachidonic acid, is a powerful chemotactic activator for granulocytes and macrophages. Two receptors for LTB4 have been identified: a high-affinity receptor (LTB4R1 or BLT1) and a low-affinity receptor (TB4R2 or BLT2). Both BLT1 and BLT2 receptors belong to the rhodopsin-like G-protein coupled receptor superfamily and primarily couple to G(i) proteins, which lead to chemotaxis, calcium mobilization, and inhibition of adenylate cyclase. In some cells, they can also couple to the Gq-like protein, G16, and activate phospholipase C. LTB4 is involved in mediating inflammatory processes, immune responses, and host defense against infection. Studies have shown that LTB4 stimulates leukocyte extravasation, neutrophil degranulation, lysozyme release, and reactive oxygen species generation. Pssm-ID: 320249 [Multi-domain] Cd Length: 278 Bit Score: 53.28 E-value: 5.90e-08
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| 7tmA_GPR119_R_insulinotropic_receptor | cd15104 | G protein-coupled receptor 119, also called glucose-dependent insulinotropic receptor, member ... |
110-325 | 6.43e-08 | |||||
G protein-coupled receptor 119, also called glucose-dependent insulinotropic receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; GPR119 is activated by oleoylethanolamide (OEA), a naturally occurring bioactive lipid with hypophagic and anti-obesity effects. Immunohistochemistry and double-immunofluorescence studies revealed the predominant GPR119 localization in pancreatic polypeptide (PP)-cells of islets. In addition, GPR119 expression is elevated in islets of obese hyperglycemic mice as compared to control islets, suggesting a possible involvement of this receptor in the development of obesity and diabetes. GPR119 has a significant sequence similarity with the members of the endothelial differentiation gene family. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320232 [Multi-domain] Cd Length: 283 Bit Score: 53.15 E-value: 6.43e-08
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| 7tmA_alpha1_AR | cd15062 | alpha-1 adrenergic receptors, member of the class A family of seven-transmembrane G ... |
79-323 | 7.05e-08 | |||||
alpha-1 adrenergic receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; The alpha-1 adrenergic receptors (or adrenoceptors) are a subfamily of the class A rhodopsin-like GPCRs that share a common architecture of seven transmembrane helices. This subfamily consists of three highly homologous receptor subtypes that primarily mediate smooth muscle contraction: alpha-1A, alpha-1B, and alpha-1D. Activation of alpha-1 receptors by catecholamines such as norepinephrine and epinephrine couples to the G(q) protein, which then activates the phospholipase C pathway, leading to an increase in IP3 and calcium. Consequently, the elevation of intracellular calcium concentration leads to vasoconstriction in smooth muscle of blood vessels. In addition, activation of alpha-1 receptors by phenylpropanolamine (PPA) produces anorexia and may induce appetite suppression in rats. Pssm-ID: 320190 [Multi-domain] Cd Length: 261 Bit Score: 52.88 E-value: 7.05e-08
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| 7tmA_GPR45 | cd15403 | G protein-coupled receptor 45, member of the class A family of seven-transmembrane G ... |
74-323 | 8.91e-08 | |||||
G protein-coupled receptor 45, member of the class A family of seven-transmembrane G protein-coupled receptors; This subgroup includes the human orphan receptor GPR45 and closely related proteins found in vertebrates. GPR45 is also called PSP24 in Xenopus and PSP24-alpha (or PSP24-1) in mammals. GPR45 shows the highest sequence homology with GPR63 (PSP24-beta, or PSP24-2). PSP24 was originally identified as a novel, high-affinity lysophosphatidic acid (LPA) receptor in Xenopus laevis oocytes; however, PSP24 receptors (GPR45 and GPR63) have not been shown to be activated by LPA. Mammalian PSP24 receptors are highly expressed in neuronal cells of cerebellum and their expression level remains constant from the early embryonic stages to adulthood, suggesting the important role of PSP24s in brain neuronal functions. Members of this subgroup contain the highly conserved Asp-Arg-Tyr/Phe (DRY/F) motif found in the third transmembrane helix (TM3) of the rhodopsin-like class A receptors which is important for efficient G protein-coupled signal transduction. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320525 [Multi-domain] Cd Length: 301 Bit Score: 52.93 E-value: 8.91e-08
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| 7tmA_HCAR1-3 | cd15201 | hydroxycarboxylic acid receptors, member of the class A family of seven-transmembrane G ... |
78-327 | 1.04e-07 | |||||
hydroxycarboxylic acid receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Hydroxycarboxylic acid receptor (HCAR) subfamily, a member of the class A G-protein coupled receptors (GPCRs), contains three receptor subtypes: HCAR1, HCAR2, and HCAR3. The endogenous ligand of HCAR1 (also known as lactate receptor 1, GPR104, or GPR81) is L-lactic acid. The endogenous ligands of HCAR2 (also known as niacin receptor 1, GPR109A, or nicotinic acid receptor) and HCAR3 (also known as niacin receptor 2 or GPR109B) are 3-hydroxybutyric acid and 3-hydroxyoctanoic acid, respectively. Because nicotinic acid is capable of stimulating HCAR2 at higher concentrations only (in the range of sub-micromolar concentration), it is unlikely that nicotinic acts as a physiological ligand of HCAR2. All three receptors are expressed in adipocytes and mediate anti-lipolytic effects in fat cells through G(i) type G protein-dependent inhibition of adenylate cyclase. Pssm-ID: 320329 [Multi-domain] Cd Length: 281 Bit Score: 52.36 E-value: 1.04e-07
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| PHA02638 | PHA02638 | CC chemokine receptor-like protein; Provisional |
106-286 | 1.05e-07 | |||||
CC chemokine receptor-like protein; Provisional Pssm-ID: 165021 [Multi-domain] Cd Length: 417 Bit Score: 53.09 E-value: 1.05e-07
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| 7tmA_PD2R2_CRTH2 | cd15118 | prostaglandin D2 receptor, member of the class A family of seven-transmembrane G ... |
82-323 | 1.16e-07 | |||||
prostaglandin D2 receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; Prostaglandin D2 receptor, also known as CRTH2, is a chemoattractant G-protein coupled receptor expressed on T helper type 2 cells that binds prostaglandin D2 (PGD2). PGD2 functions as a mast cell-derived mediator to trigger asthmatic responses and also causes vasodilation. PGD2 exerts its inflammatory effects by binding to two G-protein coupled receptors, the D-type prostanoid receptor (DP) and PD2R2 (CRTH2). PD2R2 couples to the G protein G(i/o) type which leads to a reduction in intracellular cAMP levels and an increase in intracellular calcium. PD2R2 is involved in mediating chemotaxis of Th2 cells, eosinophils, and basophils generated during allergic inflammatory processes. CRTH2 (PD2R2), but not DP receptor, undergoes agonist-induced internalization which is one of key processes that regulates the signaling of the GPCR. Pssm-ID: 320246 [Multi-domain] Cd Length: 284 Bit Score: 52.11 E-value: 1.16e-07
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| 7tmA_XCR1 | cd15182 | XC chemokine receptor 1, member of the class A family of seven-transmembrane G protein-coupled ... |
45-323 | 1.17e-07 | |||||
XC chemokine receptor 1, member of the class A family of seven-transmembrane G protein-coupled receptors; XCR1 is a chemokine receptor specific for XCL1 and XCL2 (previously called lymphotactin alpha/beta), which differ in only two amino acids. XCL1/2 is the only member of the C chemokine subfamily, which is unique as containing only two of the four cysteines that are found in other chemokine families. Human XCL1/2 has been shown to be secreted by activated CD8+ T cells and upon activation of the innate immune system. Chemokines are principal regulators for leukocyte trafficking, recruitment, and activation. Chemokine family membership is defined on the basis of sequence homology and on the presence of variations on a conserved cysteine motif, which allows the family to further divide into four subfamilies (CC, CXC, XC, and CX3C). Chemokines interact with seven-transmembrane receptors which are typically coupled to G protein for signaling. Pssm-ID: 341337 [Multi-domain] Cd Length: 271 Bit Score: 51.98 E-value: 1.17e-07
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| 7tmA_Melanopsin-like | cd15083 | vertebrate melanopsins and related opsins, member of the class A family of seven-transmembrane ... |
71-324 | 1.34e-07 | |||||
vertebrate melanopsins and related opsins, member of the class A family of seven-transmembrane G protein-coupled receptors; This group represent the Gq-coupled rhodopsin subfamily consists of melanopsins, insect photoreceptors R1-R6, invertebrate Gq opsins as well as their closely related opsins. Melanopsins (also called Opsin-4) are the primary photoreceptor molecules for non-visual functions such as the photo-entrainment of the circadian rhythm and pupillary constriction in mammals. Mammalian melanopsins are expressed only in the inner retina, whereas non-mammalian vertebrate melanopsins are localized in various extra-retinal tissues such as iris, brain, pineal gland, and skin. The outer photoreceptors (R1-R6) are the insect Drosophila equivalent to the vertebrate rods and are responsible for image formation and motion detection. The invertebrate G(q) opsins includes the arthropod and mollusk visual opsins as well as invertebrate melanopsins, which are also found in vertebrates. Arthropods possess color vision by the use of multiple opsins sensitive to different light wavelengths. Members of this subfamily belong to the class A of the G protein-coupled receptors and have seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. Pssm-ID: 320211 [Multi-domain] Cd Length: 291 Bit Score: 51.95 E-value: 1.34e-07
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| 7tmA_NTSR | cd15130 | neurotensin receptors, member of the class A family of seven-transmembrane G protein-coupled ... |
45-327 | 1.49e-07 | |||||
neurotensin receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Neurotensin (NTS) is a 13 amino-acid neuropeptide that functions as both a neurotransmitter and a hormone in the nervous system and peripheral tissues, respectively. NTS exerts various biological activities through activation of the G protein-coupled neurotensin receptors, NTSR1 and NTSR2. In the brain, NTS is involved in the modulation of dopamine neurotransmission, opioid-independent analgesia, hypothermia, and the inhibition of food intake, while in the periphery NTS promotes the growth of various normal and cancer cells and acts as a paracrine and endocrine modulator of the digestive tract. The third neurotensin receptor, NTSR3 or also called sortilin, is not a G protein-coupled receptor. Pssm-ID: 320258 [Multi-domain] Cd Length: 281 Bit Score: 51.87 E-value: 1.49e-07
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| 7tmA_GPR35_55-like | cd15923 | G protein-coupled receptor 35, GPR55, and similar proteins, member of the class A family of ... |
56-326 | 1.80e-07 | |||||
G protein-coupled receptor 35, GPR55, and similar proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This subfamily is composed of GPR35, GPR55, and similar proteins. GPR35 shares closest homology with GPR55, and they belong to the class A G protein-coupled receptor superfamily, which all have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A number of studies have suggested that GPR35 may play important physiological roles in hypertension, atherosclerosis, nociception, asthma, glucose homeostasis and diabetes, and inflammatory bowel disease. GPR35 is thought to be responsible for brachydactyly mental retardation syndrome, which is associated with a deletion comprising chromosome 2q37 in human, and is also implicated as a potential oncogene in stomach cancer. GPR35 couples to G(13) and G(i/o) proteins, whereas GPR55 has been reported to couple to G(13), G(12), or G(q) proteins. Activation of GPR55 leads to activation of phospholipase C, RhoA, ROCK, ERK, p38MAPK, and calcium release. Recently, lysophosphatidylinositol (LPI) has been identified as an endogenous ligand for GPR55, while several endogenous ligands for GPR35 have been identified including kynurenic acid, 2-oleoyl lysophosphatidic acid, and zaprinast. Pssm-ID: 320589 [Multi-domain] Cd Length: 273 Bit Score: 51.69 E-value: 1.80e-07
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| 7tmA_alpha1B_AR | cd15326 | alpha-1 adrenergic receptors subtype B, member of the class A family of seven-transmembrane G ... |
79-323 | 1.89e-07 | |||||
alpha-1 adrenergic receptors subtype B, member of the class A family of seven-transmembrane G protein-coupled receptors; The alpha-1 adrenergic receptors (or adrenoceptors) are a subfamily of the class A rhodopsin-like GPCRs that share a common architecture of seven transmembrane helices. This subfamily consists of three highly homologous receptor subtypes that primarily mediate smooth muscle contraction: alpha-1A, alpha-1B, and alpha-1D. Activation of alpha-1 receptors by catecholamines such as norepinephrine and epinephrine couples to the G(q) protein, which then activates the phospholipase C pathway, leading to an increase in IP3 and calcium. Consequently, the elevation of intracellular calcium concentration leads to vasoconstriction in smooth muscle of blood vessels. In addition, activation of alpha-1 receptors by phenylpropanolamine (PPA) produces anorexia and may induce appetite suppression in rats. Pssm-ID: 320449 [Multi-domain] Cd Length: 261 Bit Score: 51.43 E-value: 1.89e-07
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| 7tmA_alpha1A_AR | cd15325 | alpha-1 adrenergic receptors subtype A, member of the class A family of seven-transmembrane G ... |
82-323 | 1.92e-07 | |||||
alpha-1 adrenergic receptors subtype A, member of the class A family of seven-transmembrane G protein-coupled receptors; The alpha-1 adrenergic receptors (or adrenoceptors) are a subfamily of the class A rhodopsin-like GPCRs that share a common architecture of seven transmembrane helices. This subfamily consists of three highly homologous receptor subtypes that primarily mediate smooth muscle contraction: alpha-1A, alpha-1B, and alpha-1D. Activation of alpha-1 receptors by catecholamines such as norepinephrine and epinephrine couples to the G(q) protein, which then activates the phospholipase C pathway, leading to an increase in IP3 and calcium. Consequently, the elevation of intracellular calcium concentration leads to vasoconstriction in smooth muscle of blood vessels. In addition, activation of alpha-1 receptors by phenylpropanolamine (PPA) produces anorexia and may induce appetite suppression in rats. Pssm-ID: 320448 [Multi-domain] Cd Length: 261 Bit Score: 51.43 E-value: 1.92e-07
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| 7tmA_CCR10 | cd15177 | CC chemokine receptor type 10, member of the class A family of seven-transmembrane G ... |
80-325 | 1.95e-07 | |||||
CC chemokine receptor type 10, member of the class A family of seven-transmembrane G protein-coupled receptors; CCR10 is a homeostatic receptor specific for two C-C motif chemokines, CCL27 and CCL28. Activation of CCR10 by its two ligands mediates diverse activities, ranging from leukocyte trafficking to skin cancer. Chemokines are principal regulators for leukocyte trafficking, recruitment, and activation. Chemokine family membership is defined on the basis of sequence homology and on the presence of variations on a conserved cysteine motif, which allows the family to further divide into four subfamilies (CC, CXC, XC, and CX3C). Chemokines interact with seven-transmembrane receptors which are typically coupled to G protein for signaling. Currently, there are ten known receptors for CC chemokines, seven for CXC chemokines, and single receptors for the XC and CX3C chemokines. The CC chemokine receptors are all activating the G protein Gi. Pssm-ID: 341332 [Multi-domain] Cd Length: 280 Bit Score: 51.70 E-value: 1.95e-07
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| 7tmA_GPR174-like | cd15152 | putative purinergic receptor GPR174, member of the class A family of seven-transmembrane G ... |
71-327 | 2.61e-07 | |||||
putative purinergic receptor GPR174, member of the class A family of seven-transmembrane G protein-coupled receptors; GPR174 has been recently identified as a lysophosphatidylserine receptor that enhances intracellular cAMP formation by coupling to a G(s) protein. GPR174 is a member of the rhodopsin-like, class A GPCRs, which is a widespread protein family that includes the light-sensitive rhodopsin as well as receptors for biogenic amines, lipids, nucleotides, odorants, peptide hormones, and a variety of other ligands. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320280 [Multi-domain] Cd Length: 282 Bit Score: 51.26 E-value: 2.61e-07
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| 7tmA_Histamine_H3R_H4R | cd15048 | histamine receptor subtypes H3R and H4R, member of the class A family of seven-transmembrane G ... |
83-327 | 2.69e-07 | |||||
histamine receptor subtypes H3R and H4R, member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes histamine subtypes H3R and H4R, members of the histamine receptor family, which belong to the class A of GPCRs. Histamine plays a key role as chemical mediator and neurotransmitter in various physiological and pathophysiological processes in the central and peripheral nervous system. Histamine exerts its functions by binding to four different G protein-coupled receptors (H1-H4). The H3 and H4 receptors couple to the G(i)-proteins, which leading to the inhibition of cAMP formation. The H3R receptor functions as a presynaptic autoreceptors controlling histamine release and synthesis. The H4R plays an important role in histamine-mediated chemotaxis in mast cells and eosinophils. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320176 [Multi-domain] Cd Length: 296 Bit Score: 51.15 E-value: 2.69e-07
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| 7tmA_mAChR | cd15049 | muscarinic acetylcholine receptor subfamily, member of the class A family of ... |
83-323 | 2.82e-07 | |||||
muscarinic acetylcholine receptor subfamily, member of the class A family of seven-transmembrane G protein-coupled receptors; Muscarinic acetylcholine receptors (mAChRs) regulate the activity of many fundamental central and peripheral functions. The mAChR family consists of 5 subtypes M1-M5, which can be further divided into two major groups according to their G-protein coupling preference. The M1, M3 and M5 receptors selectively interact with G proteins of the G(q/11) family, whereas the M2 and M4 receptors preferentially link to the G(i/o) types of G proteins. Activation of mAChRs by agonist (acetylcholine) leads to a variety of biochemical and electrophysiological responses. In general, the exact nature of these responses and the subsequent physiological effects mainly depend on the molecular and pharmacological identity of the activated receptor subtype(s). All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 341322 [Multi-domain] Cd Length: 262 Bit Score: 50.78 E-value: 2.82e-07
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| 7tmA_PrRP_R | cd15394 | prolactin-releasing peptide receptor, member of the class A family of seven-transmembrane G ... |
107-323 | 2.84e-07 | |||||
prolactin-releasing peptide receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; Prolactin-releasing peptide (PrRP) receptor (previously known as GPR10) is expressed in the central nervous system with the highest levels located in the anterior pituitary and is activated by its endogenous ligand PrRP, a neuropeptide possessing a C-terminal Arg-Phe-amide motif. There are two active isoforms of PrRP in mammals: one consists of 20 amino acids (PrRP-20) and the other consists of 31 amino acids (PrRP-31), where PrRP-20 is a C-terminal fragment of PrRP-31. Binding of PrRP to the receptor coupled to G(i/o) proteins activates the extracellular signal-related kinase (ERK) and it can also couple to G(q) protein leading to an increase in intracellular calcium and activation of c-Jun N-terminal protein kinase (JNK). The PrRP receptor shares significant sequence homology with the neuropeptide Y (NPY) receptor, and micromolar levels of NPY can bind and completely inhibit the PrRP-evoked intracellular calcium response in PrRP receptor-expressing cells, suggesting that the PrRP receptor shares a common ancestor with the NPY receptors. PrRP has been shown to reduce food intake and body weight and modify body temperature when administered in rats. It also has been shown to decrease circulating growth hormone levels by activating somatostatin-secreting neurons in the hypothalamic periventricular nucleus. Pssm-ID: 320516 [Multi-domain] Cd Length: 286 Bit Score: 51.28 E-value: 2.84e-07
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| 7tmA_Adenosine_R_A2B | cd15069 | adenosine receptor subtype 2AB, member of the class A family of seven-transmembrane G ... |
114-325 | 3.46e-07 | |||||
adenosine receptor subtype 2AB, member of the class A family of seven-transmembrane G protein-coupled receptors; The A2B receptor, a member of the adenosine receptor family of G protein-coupled receptors, binds adenosine as its endogenous ligand and is involved in regulating myocardial oxygen consumption and coronary blood flow. High-affinity A2A and low-affinity A2B receptors are preferentially coupled to G proteins of the stimulatory (Gs) family, which lead to activation of adenylate cyclase and thereby increasing the intracellular cAMP levels. The A2A receptor activation protects against tissue injury and acts as anti-inflammatory agent. In human skin endothelial cells, activation of A2B receptor, but not the A2A receptor, promotes angiogenesis. Alternatively, activated A2A receptor, but not the A2B receptor, promotes angiogenesis in human umbilical vein and lung microvascular endothelial cells. The A2A receptor alters cardiac contractility indirectly by modulating the anti-adrenergic effect of A1 receptor, while the A2B receptor exerts direct effects on cardiac contractile function, but does not modulate beta-adrenergic or A1 anti-adrenergic effects. Pssm-ID: 320197 [Multi-domain] Cd Length: 294 Bit Score: 51.09 E-value: 3.46e-07
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| 7tmA_GPR34-like | cd15148 | putative G protein-coupled receptor 34, member of the class A family of seven-transmembrane G ... |
72-327 | 3.81e-07 | |||||
putative G protein-coupled receptor 34, member of the class A family of seven-transmembrane G protein-coupled receptors; This subgroup represents the G-protein coupled receptor 34 of unknown function. Orphan GPR34 is a member of the rhodopsin-like, class A GPCRs, which is a widespread protein family that includes the light-sensitive rhodopsin as well as receptors for biogenic amines, lipids, nucleotides, odorants, peptide hormones, and a variety of other ligands. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320276 [Multi-domain] Cd Length: 282 Bit Score: 50.85 E-value: 3.81e-07
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| 7tmA_5-HT5 | cd15328 | serotonin receptor subtype 5, member of the class A family of seven-transmembrane G ... |
79-327 | 3.84e-07 | |||||
serotonin receptor subtype 5, member of the class A family of seven-transmembrane G protein-coupled receptors; 5-HT5 receptor, one of 14 mammalian 5-HT receptors, is activated by the neurotransmitter and peripheral signal mediator serotonin (also known as 5-hydroxytryptamine or 5-HT). The 5-HT5A and 5-HT5B receptors have been cloned from rat and mouse, but only the 5-HT5A isoform has been identified in human because of the presence of premature stop codons in the human 5-HT5B gene, which prevents a functional receptor from being expressed. 5-HT5 receptors mediate inhibitory neurotransmission by coupling to G proteins of the G(i/0) family, which lead to a decrease in adenylate cyclase activity, thereby decreasing intracellular cAMP levels and calcium influx. In the CNS, serotonin is involved in the regulation of appetite, mood, sleep, cognition, learning and memory, as well as implicated in neurologic disorders such as migraine, schizophrenia, and depression. Pssm-ID: 320451 [Multi-domain] Cd Length: 259 Bit Score: 50.72 E-value: 3.84e-07
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| 7tmA_BNGR-A34-like | cd15000 | putative neuropeptide receptor BNGR-A34 and similar proteins, member of the class A family of ... |
78-325 | 4.02e-07 | |||||
putative neuropeptide receptor BNGR-A34 and similar proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This subgroup includes putative neuropeptide receptor BNGR-A34 found in silkworm and its closely related proteins from invertebrates. They are members of the class A rhodopsin-like GPCRs, which represent a widespread protein family that includes the light-sensitive rhodopsin as well as receptors for biogenic amines, lipids, nucleotides, odorants, peptide hormones, and a variety of other ligands. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320131 [Multi-domain] Cd Length: 285 Bit Score: 50.50 E-value: 4.02e-07
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| 7tmA_Beta1_AR | cd15958 | beta-1 adrenergic receptors (adrenoceptors), member of the class A family of ... |
78-323 | 4.73e-07 | |||||
beta-1 adrenergic receptors (adrenoceptors), member of the class A family of seven-transmembrane G protein-coupled receptors; The beta-1 adrenergic receptor (beta-1 adrenoceptor), also known as beta-1 AR, is activated by adrenaline (epinephrine) and plays important roles in regulating cardiac function and heart rate. The human heart contains three subtypes of the beta AR: beta-1 AR, beta-2 AR, and beta-3 AR. Beta-1 AR and beta-2 AR, which expressed at about a ratio of 70:30, are the major subtypes involved in modulating cardiac contractility and heart rate by positively stimulating the G(s) protein-adenylate cyclase-cAMP-PKA signaling pathway. In contrast, beta-3 AR produces negative inotropic effects by activating inhibitory G(i) proteins. The aberrant expression of betrayers can lead to cardiac dysfunction such as arrhythmias or heart failure. Pssm-ID: 320624 [Multi-domain] Cd Length: 298 Bit Score: 50.67 E-value: 4.73e-07
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| 7tmA_CysLTR | cd15921 | cysteinyl leukotriene receptors, member of the class A family of seven-transmembrane G ... |
106-327 | 6.64e-07 | |||||
cysteinyl leukotriene receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Cysteinyl leukotrienes (LTC4, LTD4, and LTE4) are the most potent inflammatory lipid mediators that play an important role in human asthma. They are synthesized in the leucocytes (cells of immune system) from arachidonic acid by the actions of 5-lipoxygenase and induce bronchial constriction through G protein-coupled receptors, CysLTR1 and CysLTR2. Activation of CysLTR1 by LTD4 induces airway smooth muscle contraction and proliferation, eosinophil migration, and damage to the lung tissue. They belong to the class A GPCR superfamily, which all have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320587 [Multi-domain] Cd Length: 283 Bit Score: 49.81 E-value: 6.64e-07
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| 7tmA_SSTR2 | cd15971 | somatostatin receptor type 2, member of the class A family of seven-transmembrane G ... |
95-327 | 7.02e-07 | |||||
somatostatin receptor type 2, member of the class A family of seven-transmembrane G protein-coupled receptors; G protein-coupled somatostatin receptors (SSTRs), which display strong sequence similarity with opioid receptors, binds somatostatin, a polypeptide hormone that regulates a wide variety of physiological such as neurotransmission, endocrine secretion, cell proliferation, and smooth muscle contractility. SSTRs are composed of five distinct subtypes (SSTR1-5) which are encoded by separate genes on different chromosomes. SSTR2 plays critical roles in growth hormone secretion, glucagon secretion, and immune responses. SSTR2 is expressed in the normal human pituitary and in nearly all pituitary growth hormone adenomas. Pssm-ID: 320637 [Multi-domain] Cd Length: 279 Bit Score: 49.84 E-value: 7.02e-07
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| 7tmA_alpha2A_AR | cd15322 | alpha-2 adrenergic receptors subtype A, member of the class A family of seven-transmembrane G ... |
78-327 | 7.96e-07 | |||||
alpha-2 adrenergic receptors subtype A, member of the class A family of seven-transmembrane G protein-coupled receptors; The alpha-2 adrenergic receptors (or adrenoceptors) are a subfamily of the class A rhodopsin-like GPCRs that share a common architecture of seven transmembrane helices. This subfamily consists of three highly homologous receptor subtypes that have a key role in neurotransmitter release: alpha-2A, alpha-2B, and alpha-2C. In addition, a fourth subtype, alpha-2D is present in ray-finned fishes and amphibians, but is not found in humans. The alpha-2 receptors are found in both central and peripheral nervous system and serve to produce inhibitory functions through the G(i) proteins. Thus, the alpha-2 receptors inhibit adenylate cyclase, which decreases cAMP production and thereby decreases calcium influx during the action potential. Consequently, lowered levels of calcium will lead to a decrease in neurotransmitter release by negative feedback. Pssm-ID: 320445 [Multi-domain] Cd Length: 259 Bit Score: 49.56 E-value: 7.96e-07
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| 7tmA_NAGly_R_GPR18 | cd15166 | N-arachidonyl glycine receptor, GPR18, member of the class A family of seven-transmembrane G ... |
92-285 | 8.38e-07 | |||||
N-arachidonyl glycine receptor, GPR18, member of the class A family of seven-transmembrane G protein-coupled receptors; N-arachidonyl glycine (NAGly), an endogenous metabolite of the endocannabinoid anandamide, has been identified as an endogenous ligand of the G(i/o) protein-coupled receptor 18 (GPR18). NAGly is involved in directing microglial migration in the CNS through activation of GPR18. NAGly-GPR18 signaling is thought to play an important role in microglial-neuronal communication. Recent studies also show that GPR18 functions as the abnormal cannabidiol (Abn-CBD) receptor. Abn-CBD is a synthetic isomer of cannabidiol and is inactive at cannabinoid receptors (CB1 or CB2), but acts as a selective agonist at GPR18. The NAGly receptor is a member of the class A G protein-coupled receptor superfamily, which all have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, which then activate the heterotrimeric G proteins. G-proteins regulate a variety of cellular functions including metabolic enzymes, ion channels, and transporters, among many others. Pssm-ID: 320294 [Multi-domain] Cd Length: 275 Bit Score: 49.43 E-value: 8.38e-07
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| 7tmA_ACKR2_D6 | cd15188 | atypical chemokine receptor 2, member of the class A family of seven-transmembrane G ... |
45-327 | 9.31e-07 | |||||
atypical chemokine receptor 2, member of the class A family of seven-transmembrane G protein-coupled receptors; ACKR2 (also known as D6) binds non-selectively to all inflammatory CC-chemokines, but not to homeostatic CC-chemokines involved in controlling the migration of cells. Unlike the classical chemokine receptors that contain a conserved DRYLAIV motif in the second intracellular loop, which is required for G-protein coupling, the ACKRs lack this conserved motif and fail to couple to G-proteins and induce classical GPCR signaling. Five receptors have been identified for the ACKR family, including CC-chemokine receptors like 1 and 2 (CCRL1 and CCRL2), CXCR7, Duffy antigen receptor for chemokine (DARC), and D6. Both ACKR1 (DARC) and ACKR3 (CXCR7) show low sequence homology to the classic chemokine receptors. Pssm-ID: 320316 [Multi-domain] Cd Length: 278 Bit Score: 49.40 E-value: 9.31e-07
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| 7tmA_HCAR-like | cd14991 | hydroxycarboxylic acid receptors and related proteins, member of the class A family of ... |
107-327 | 9.52e-07 | |||||
hydroxycarboxylic acid receptors and related proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes the hydroxycarboxylic acid receptors (HCARs) as well as their closely related receptors, GPR31 and oxoeicosanoid receptor 1 (OXER1). HCARs are members of the class A family of G-protein coupled receptors (GPCRs). HCAR subfamily contain three receptor subtypes: HCAR1, HCAR2, and HCAR3. The endogenous ligand of HCAR1 (also known as lactate receptor 1, GPR104, or GPR81) is L-lactic acid. The endogenous ligands of HCAR2 (also known as niacin receptor 1, GPR109A, nicotinic acid receptor) and HCAR3 (also known as niacin receptor 2, orGPR109B) are 3-hydroxybutyric acid and 3-hydroxyoctanoic acid, respectively. All three HCA receptors are expressed in adipocytes, and are coupled to G(i)-proteins mediating anti-lipolytic effects in fat cells. OXER1 is a receptor for eicosanoids and polyunsaturated fatty acids such as 5-oxo-6E,8Z,11Z,14Z-eicosatetraenoic acid (5-OXO-ETE), 5(S)-hydroperoxy-6E,8Z,11Z,14Z-eicosatetraenoic acid (5(S)-HPETE) and arachidonic acid, whereas GPR31 is a high-affinity receptor for 12-(S)-hydroxy-5,8,10,14-eicosatetraenoic acid (12-S-HETE). Pssm-ID: 320122 [Multi-domain] Cd Length: 280 Bit Score: 49.37 E-value: 9.52e-07
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| 7tmA_OXGR1 | cd15375 | 2-oxoglutarate receptor 1, member of the class A family of seven-transmembrane G ... |
107-286 | 1.01e-06 | |||||
2-oxoglutarate receptor 1, member of the class A family of seven-transmembrane G protein-coupled receptors; 2-oxoglutarate receptor 1 (OXGR1) is also known as GPR80, GPR99, or P2Y15. OXGR1 functions as a receptor for alpha-ketoglutarate, a citric acid cycle intermediate, and acts exclusively through a G(q)-dependent pathway. OXGR1 belongs to the class A GPCR superfamily and is phylogenetically related to the purinergic P2Y1-like receptor subfamily, whose members are coupled to G(q) protein to activate phospholipase C (PLC). OXGR1 has also been reported as a potential third cysteinyl leukotriene receptor with specificity for leukotriene E4. Pssm-ID: 320497 [Multi-domain] Cd Length: 280 Bit Score: 49.30 E-value: 1.01e-06
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| 7tmA_FFAR2_FFAR3 | cd15170 | free fatty acid receptors 2, 3, and similar proteins, member of the class A family of ... |
72-327 | 1.16e-06 | |||||
free fatty acid receptors 2, 3, and similar proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; This subgroup includes free fatty acid receptor 2 (FFAR2), FFAR3, and similar proteins. They are a member of the class A G-protein coupled receptors that bind free fatty acids. The FFAR subfamily is composed of three receptors, each encoded by a separate gene (FFAR1, FFAR2, and FFAR3). These genes and a fourth pseudogene, GPR42, are localized together on chromosome 19. FFAR2 and FFAR3 are cell-surface receptors for short chain FFAs (SCFAs) with different ligand affinities, whereas FFAR1 is a receptor for medium- and long-chain FFAs. FFAR2 activation by SCFA suppresses adipose insulin signaling, which leads to inhibition of fat accumulation in adipose tissue. FAAR3 is expressed in intestinal L cells, which produces glucagon-like peptide 1 (GLP-1) and peptide YY (PYY), thus suggesting that this receptor may be involved in energy homeostasis. FFARs are considered important components of the body's nutrient sensing mechanism, and therefore, these receptors are potential therapeutic targets for the treatment of metabolic disorders, such as type 2 diabetes and obesity. Pssm-ID: 320298 Cd Length: 278 Bit Score: 49.18 E-value: 1.16e-06
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| 7tmA_Mel1A | cd15402 | melatonin receptor subtype 1A, member of the class A family of seven-transmembrane G ... |
83-324 | 1.49e-06 | |||||
melatonin receptor subtype 1A, member of the class A family of seven-transmembrane G protein-coupled receptors; Melatonin (N-acetyl-5-methoxytryptamine) is a naturally occurring sleep-promoting chemical found in vertebrates, invertebrates, bacteria, fungi, and plants. In mammals, melatonin is secreted by the pineal gland and is involved in regulation of circadian rhythms. Its production peaks during the nighttime, and is suppressed by light. Melatonin is shown to be synthesized in other organs and cells of many vertebrates, including the Harderian gland, leukocytes, skin, and the gastrointestinal (GI) tract, which contains several hundred times more melatonin than the pineal gland and is involved in the regulation of GI motility, inflammation, and sensation. Melatonin exerts its pleiotropic physiological effects through specific membrane receptors, named MT1A, MT1B, and MT1C, which belong to the class A rhodopsin-like G-protein coupled receptor family. MT1A and MT1B subtypes are present in mammals, whereas MT1C subtype has been found in amphibians and birds. The melatonin receptors couple to G proteins of the G(i/o) class, leading to the inhibition of adenylate cyclase. Pssm-ID: 320524 [Multi-domain] Cd Length: 279 Bit Score: 48.75 E-value: 1.49e-06
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| 7tmA_LPAR6_P2Y5 | cd15156 | lysophosphatidic acid receptor 6, member of the class A family of seven-transmembrane G ... |
82-327 | 1.49e-06 | |||||
lysophosphatidic acid receptor 6, member of the class A family of seven-transmembrane G protein-coupled receptors; Lysophosphatidic acid receptor 6 (LPAR6), also known as P2Y5, is a G(i), G(12/13) G protein-coupled receptor that is activated by the bioactive lipid lysophosphatidic acid (LPA), which is released by activated platelets and constitutively present in serum. LPAR6 plays an important role in maintenance of human hair growth. Thus, mutations in the receptor are responsible for both autosomal recessive wooly hair and hypotrichosis. Phylogenetic analysis of the class A GPCRs shows that LAPR6 (P2Y5) is classified into the cluster consisting of receptors that are preferentially activated by adenosine and uridine nucleotides. Although LPA6 (P2Y5) is expressed in human hair follicle cells, LPA4 and LPA5 are not. These three receptors are highly homologous and mediate an increase in intracellular cAMP production. Pssm-ID: 320284 [Multi-domain] Cd Length: 285 Bit Score: 49.08 E-value: 1.49e-06
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| 7tmA_CCR1 | cd15183 | CC chemokine receptor type 1, member of the class A family of seven-transmembrane G ... |
107-285 | 1.62e-06 | |||||
CC chemokine receptor type 1, member of the class A family of seven-transmembrane G protein-coupled receptors; CCR1 is widely expressed on both hematopoietic and non-hematopoietic cells and binds to the inflammatory CC chemokines CCL3, CCL5, CCL6, CCL9, CCL15, and CCL23. CCR1 activates the typical chemokine signaling pathway through the G(i/o) type of G proteins, causing inhibition of adenylate cyclase and stimulation of phospholipase C, PKC, calcium flux, and PLA2. Chemokines are principal regulators for leukocyte trafficking, recruitment, and activation. Chemokine family membership is defined on the basis of sequence homology and on the presence of variations on a conserved cysteine motif, which allows the family to further divide into four subfamilies (CC, CXC, XC, and CX3C). Chemokines interact with seven-transmembrane receptors which are typically coupled to G protein for signaling. Currently, there are ten known receptors for CC chemokines, seven for CXC chemokines, and single receptors for the XC and CX3C chemokines. Pssm-ID: 320311 [Multi-domain] Cd Length: 278 Bit Score: 48.71 E-value: 1.62e-06
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| 7tmA_GPR55-like | cd15165 | G protein-coupled receptor 55 and similar proteins, member of the class A family of ... |
46-328 | 1.77e-06 | |||||
G protein-coupled receptor 55 and similar proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; GPR55 shares closest homology with GPR35, and they belong to the class A G protein-coupled receptor superfamily, which all have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. GPR55 has been reported to couple to G(13), G(12), or G(q) proteins. Activation of GPR55 leads to activation of phospholipase C, RhoA, ROCK, ERK, p38MAPK, and calcium release. Lysophosphatidylinositol (LPI) is currently considered as the endogenous ligand for GPR55, although the receptor was initially de-orphanized as a cannabinoid receptor and binds many cannabinoid ligands. Pssm-ID: 320293 [Multi-domain] Cd Length: 277 Bit Score: 48.48 E-value: 1.77e-06
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| 7tmA_ACKR4_CCR11 | cd15176 | atypical chemokine receptor 4, member of the class A family of seven-transmembrane G ... |
71-293 | 1.90e-06 | |||||
atypical chemokine receptor 4, member of the class A family of seven-transmembrane G protein-coupled receptors; ACKR4 was first reported to bind several CC chemokines including CCL19, CCL21, and CCL25 and was originally designated CCR11. AKCR4 is unable to couple to G-protein and, instead, it preferentially mediates beta-arrestin dependent processes, such as receptor internalization, after ligand binding. Thus, ACKR4 may act as a scavenger receptor to suppress the effects of proinflammatory chemokines. Unlike the classical chemokine receptors that contain a conserved DRYLAIV motif in the second intracellular loop, which is required for G-protein coupling, the ACKRs lack this conserved motif and fail to couple to G-proteins and induce classical GPCR signaling. Five receptors have been identified for the ACKR family, including CC-chemokine receptors like 1 and 2 (CCRL1 and CCRL2), CXCR7, Duffy antigen receptor for chemokine (DARC), and D6. Both ACKR1 (DARC) and ACKR3 (CXCR7) show low sequence homology to the classic chemokine receptors. Pssm-ID: 320304 [Multi-domain] Cd Length: 276 Bit Score: 48.59 E-value: 1.90e-06
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| 7tmA_motilin_R | cd15132 | motilin receptor, member of the class A family of seven-transmembrane G protein-coupled ... |
37-327 | 2.02e-06 | |||||
motilin receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; Motilin receptor, also known as GPR38, is a G-protein coupled receptor that binds the endogenous ligand motilin. Motilin is a 22 amino acid peptide hormone expressed throughout the gastrointestinal tract and stimulates contraction of gut smooth muscle. Motilin is also called as the housekeeper of the gut because it is responsible for the proper filling and emptying of the gastrointestinal tract in response to food intake, and for stimulating the production of pepsin. Motilin receptor shares significant amino acid sequence identity with the growth hormone secretagogue receptor (GHSR) and neurotensin receptors (NTS-R1 and 2). Pssm-ID: 320260 [Multi-domain] Cd Length: 289 Bit Score: 48.64 E-value: 2.02e-06
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| 7tmA_PAR2 | cd15370 | protease-activated receptor 2, member of the class A family of seven-transmembrane G ... |
71-327 | 2.26e-06 | |||||
protease-activated receptor 2, member of the class A family of seven-transmembrane G protein-coupled receptors; Protease-acted receptors (PARs) are seven-transmembrane proteins that belong to the class A G-protein coupled receptor (GPCR) family. Four different types of the protease-activated receptors have been identified: PAR1, PAR2, PAR3, and PAR4. PARs are predominantly expressed in platelets and are activated by serine proteases such as thrombin, trypsin, and tryptase. These proteases cleave the extracellular domain of the receptor to form a new N-terminus, which in turn functions as a tethered ligand. The newly-formed tethered ligand binds intramolecularly to activate the receptor and triggers G-protein binding and intracellular signaling. PAR1, PA3, and PAR4 are activated by thrombin, whereas PAR2 is activated by trypsin. The PARs are known to couple with several G-proteins including Gi (cAMP inhibitory), G12/13 (Rho and Ras activation), and Gq (calcium signaling) to activate downstream signaling messengers which induces numerous cellular and physiological effects. Pssm-ID: 341349 [Multi-domain] Cd Length: 280 Bit Score: 48.25 E-value: 2.26e-06
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| 7tmA_LPAR5 | cd15154 | lysophosphatidic acid receptor 5, member of the class A family of seven-transmembrane G ... |
71-327 | 2.28e-06 | |||||
lysophosphatidic acid receptor 5, member of the class A family of seven-transmembrane G protein-coupled receptors; Lysophosphatidic acid receptor 5 (LPAR5) is a G protein-coupled receptor that binds the bioactive lipid lysophosphatidic acid (LPA) and is involved in maintenance of human hair growth. Phylogenetic analysis of the class A GPCRs shows that LAPR5 is classified into the cluster consisting receptors that are preferentially activated by adenosine and uridine nucleotides. Although LPA6 (P2Y5) is expressed in human hair follicle cells, LPA4 and LPA5 are not. These three receptors are highly homologous and mediate an increase in intracellular cAMP production. Activation of LPAR5 is coupled to G(q) and G(12/13) proteins. Pssm-ID: 320282 [Multi-domain] Cd Length: 285 Bit Score: 48.22 E-value: 2.28e-06
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| 7tmA_Parietopsin | cd15085 | non-visual parietopsins, member of the class A family of seven-transmembrane G protein-coupled ... |
132-323 | 2.63e-06 | |||||
non-visual parietopsins, member of the class A family of seven-transmembrane G protein-coupled receptors; Parietopsin is a non-visual green light-sensitive opsin that was initially identified in the parietal eye of lizards. The vertebrate non-visual opsin family includes pinopsins, parapinopsin, VA (vertebrate ancient) opsins, and parietopsins. These non-visual opsins are expressed in various extra-retinal tissues and/or in non-rod, non-cone retinal cells. They are thought to be involved in light-dependent physiological functions such as photo-entrainment of circadian rhythm, photoperiodicity and body color change. Parietopsin belongs to the class A of the G protein-coupled receptors and shows strong homology to the vertebrate visual opsins. Pssm-ID: 320213 [Multi-domain] Cd Length: 280 Bit Score: 48.31 E-value: 2.63e-06
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| 7tmA_5-HT1E | cd15335 | serotonin receptor subtype 1E, member of the class A family of seven-transmembrane G ... |
79-327 | 2.74e-06 | |||||
serotonin receptor subtype 1E, member of the class A family of seven-transmembrane G protein-coupled receptors; The 5-HT1 receptors, one of 14 mammalian 5-HT receptors, is a member of the class A of GPCRs and is activated by the endogenous neurotransmitter and peripheral signal mediator serotonin (5-hydroxytryptamine, 5-HT). The 5-HT1 receptors mediate inhibitory neurotransmission by coupling to G proteins of the G(i/o) family, which lead to a decrease in adenylate cyclase activity, thereby decreasing intracellular cAMP levels and calcium influx. The 5-HT1 receptor subfamily includes 5 subtypes: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F. There is no 5-HT1C receptor subtype, as it has been reclassified as the 5-HT2C receptor. In the CNS, serotonin is involved in the regulation of appetite, mood, sleep, cognition, learning and memory, as well as implicated in neurologic disorders such as migraine, schizophrenia, and depression. Pssm-ID: 320457 [Multi-domain] Cd Length: 258 Bit Score: 48.00 E-value: 2.74e-06
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| 7tmA_GPR35-like | cd15164 | G protein-coupled receptor 35 and similar proteins, member of the class A family of ... |
45-326 | 2.96e-06 | |||||
G protein-coupled receptor 35 and similar proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; GPR35 shares closest homology with GPR55, and they belong to the class A G protein-coupled receptor superfamily, which all have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A number of studies have suggested that GPR35 may play important physiological roles in hypertension, atherosclerosis, nociception, asthma, glucose homeostasis and diabetes, and inflammatory bowel disease. GPR35 is thought to be responsible for brachydactyly mental retardation syndrome, which is associated with a deletion comprising chromosome 2q37 in human, and is also implicated as a potential oncogene in stomach cancer. Several endogenous ligands for GPR35 have been identified including kynurenic acid, 2-oleoyl lysophosphatidic acid, and zaprinast. GPR35 couples to G(13) and G(i/o) proteins. Pssm-ID: 320292 [Multi-domain] Cd Length: 272 Bit Score: 48.03 E-value: 2.96e-06
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| 7tmA_TRH-R | cd14995 | thyrotropin-releasing hormone receptor, member of the class A family of seven-transmembrane G ... |
92-327 | 3.86e-06 | |||||
thyrotropin-releasing hormone receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; TRH-R is a member of the class A rhodopsin-like G protein-coupled receptors, which binds the tripeptide thyrotropin releasing hormone. The TRH-R activates phosphoinositide metabolism through a pertussis-toxin-insensitive G-protein, the G(q)/G(11) class. TRH stimulates the synthesis and release of thyroid-stimulating hormone in the anterior pituitary. TRH is produced in many other tissues, especially within the nervous system, where it appears to act as a neurotransmitter/neuromodulator. It also stimulates the synthesis and release of prolactin. In the CNS, TRH stimulates a number of behavioral and pharmacological actions, including increased turnover of catecholamines in the nucleus accumbens. There are two thyrotropin-releasing hormone receptors in some mammals, thyrotropin-releasing hormone receptor 1 (TRH1) which has been found in a number of species including rat, mouse, and human and thyrotropin-releasing hormone receptor 2 (TRH2) which has, only been found in rodents. These TRH receptors are found in high levels in the anterior pituitary, and are also found in the retina and in certain areas of the brain. Pssm-ID: 320126 [Multi-domain] Cd Length: 269 Bit Score: 47.38 E-value: 3.86e-06
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| 7tmA_DmOct-betaAR-like | cd15066 | Drosophila melanogaster beta-adrenergic receptor-like octopamine receptors and similar ... |
83-326 | 3.91e-06 | |||||
Drosophila melanogaster beta-adrenergic receptor-like octopamine receptors and similar receptors in bilateria; member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes Drosophila beta-adrenergic-like octopamine receptors and similar proteins. The biogenic amine octopamine is the invertebrate equivalent of vertebrate adrenergic neurotransmitters and exerts its effects through different G protein-coupled receptor types. Insect octopamine receptors are involved in the modulation of carbohydrate metabolism, muscular tension, cognition and memory. The activation of octopamine receptors mediating these actions leads to an increase in adenylate cyclase activity, thereby increasing cAMP levels. In Drosophila melanogaster, three subgroups have been classified on the basis of their structural homology and functional equivalents with vertebrate beta-adrenergic receptors: DmOctBeta1R, DmOctBeta2R, and DmOctBeta3R. Pssm-ID: 320194 [Multi-domain] Cd Length: 265 Bit Score: 47.37 E-value: 3.91e-06
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| 7tmA_Mel1 | cd15209 | melatonin receptor 1, member of the class A family of seven-transmembrane G protein-coupled ... |
69-324 | 3.96e-06 | |||||
melatonin receptor 1, member of the class A family of seven-transmembrane G protein-coupled receptors; Melatonin (N-acetyl-5-methoxytryptamine) is a naturally occurring sleep-promoting chemical found in vertebrates, invertebrates, bacteria, fungi, and plants. In mammals, melatonin is secreted by the pineal gland and is involved in regulation of circadian rhythms. Its production peaks during the nighttime, and is suppressed by light. Melatonin is shown to be synthesized in other organs and cells of many vertebrates, including the Harderian gland, leukocytes, skin, and the gastrointestinal (GI) tract, which contains several hundred times more melatonin than the pineal gland and is involved in the regulation of GI motility, inflammation, and sensation. Melatonin exerts its pleiotropic physiological effects through specific membrane receptors, named MT1A, MT1B, and MT1C, which belong to the class A rhodopsin-like G-protein coupled receptor family. MT1A and MT1B subtypes are present in mammals, whereas MT1C subtype has been found in amphibians and birds. The melatonin receptors couple to G proteins of the G(i/o) class, leading to the inhibition of adenylate cyclase. Pssm-ID: 320337 [Multi-domain] Cd Length: 279 Bit Score: 47.47 E-value: 3.96e-06
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| 7tmA_Opsin_Gq_invertebrates | cd15337 | invertebrate Gq opsins, member of the class A family of seven-transmembrane G protein-coupled ... |
132-323 | 4.62e-06 | |||||
invertebrate Gq opsins, member of the class A family of seven-transmembrane G protein-coupled receptors; The invertebrate Gq-coupled opsin subfamily includes the arthropod and mollusc visual opsins. Like the vertebrate visual opsins, arthropods possess color vision by the use of multiple opsins sensitive to different light wavelengths. The invertebrate Gq opsins are closely related to the vertebrate melanopsins, the primary photoreceptor molecules for non-visual responses to light, and the R1-R6 photoreceptors, which are the fly equivalent to the vertebrate rods. The Gq opsins belong the class A of the G protein-coupled receptors and possess seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. Pssm-ID: 320459 [Multi-domain] Cd Length: 292 Bit Score: 47.32 E-value: 4.62e-06
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| 7tmA_CysLTR2 | cd15157 | cysteinyl leukotriene receptor 2, member of the class A family of seven-transmembrane G ... |
107-327 | 4.91e-06 | |||||
cysteinyl leukotriene receptor 2, member of the class A family of seven-transmembrane G protein-coupled receptors; Cysteinyl leukotrienes (LTC4, LTD4, and LTE4) are the most potent inflammatory lipid mediators that play an important role in human asthma. They are synthesized in the leucocytes (cells of immune system) from arachidonic acid by the actions of 5-lipoxygenase and induce bronchial constriction through G protein-coupled receptors, CysLTR1 and CysLTR2. Activation of CysLTR1 by LTD4 induces airway smooth muscle contraction and proliferation, eosinophil migration, and damage to the lung tissue. They belong to the class A GPCR superfamily, which all have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320285 [Multi-domain] Cd Length: 278 Bit Score: 47.40 E-value: 4.91e-06
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| 7tmA_AstC_insect | cd15094 | somatostatin-like receptor for allatostatin C, member of the class A family of ... |
107-327 | 6.66e-06 | |||||
somatostatin-like receptor for allatostatin C, member of the class A family of seven-transmembrane G protein-coupled receptors; G protein-coupled somatostatin receptors (SSTRs) are composed of five distinct subtypes (SSTR1-5) that display strong sequence similarity with opioid receptors. All five receptor subtypes bind the natural somatostatin (somatotropin release inhibiting factor), a polypeptide hormone that regulates a wide variety of physiological functions such as neurotransmission, cell proliferation, contractility of smooth muscle cells, and endocrine signaling as well as inhibition of the release of many secondary hormones. In Drosophila melanogaster and other insects, a 15-amino-acid peptide named allatostatin C(AstC) binds the somatostatin-like receptors. Two AstC receptors have been identified in Drosophila with strong sequence homology to human somatostatin and opioid receptors. Pssm-ID: 320222 [Multi-domain] Cd Length: 282 Bit Score: 47.08 E-value: 6.66e-06
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| 7tmA_GHSR | cd15131 | growth hormone secretagogue receptor, member of the class A family of seven-transmembrane G ... |
39-285 | 8.24e-06 | |||||
growth hormone secretagogue receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; Growth hormone secretagogue receptor, GHSR, is also known as GH-releasing peptide receptor (GHRP) or Ghrelin receptor. Ghrelin, the endogenous ligand for GHSR, is an acylated 28-amino acid peptide hormone produced by ghrelin cells in the gastrointestinal tract. Ghrelin, also called hunger hormone, is involved in the regulation of growth hormone release, appetite and feeding, gut motility, lipid and glucose metabolism, and energy balance. It also plays a role in the cardiovascular, immune, and reproductive systems. GHSR couples to G-alpha-11 proteins. Both ghrelin and GHSR are expressed in a wide range of cancer tissues. Recent studies suggested that ghrelin may play a role in processes associated with cancer progression, including cell proliferation, metastasis, apoptosis, and angiogenesis. Pssm-ID: 320259 [Multi-domain] Cd Length: 291 Bit Score: 46.80 E-value: 8.24e-06
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| 7tmA_D1B_dopamine_R | cd15319 | D1B (or D5) subtype dopamine receptor, member of the class A family of seven-transmembrane G ... |
83-325 | 8.91e-06 | |||||
D1B (or D5) subtype dopamine receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; Dopamine receptors are members of the class A G protein-coupled receptors that are involved in many neurological processes in the central nervous system (CNS). The neurotransmitter dopamine is the primary endogenous agonist for dopamine receptors. Dopamine receptors consist of at least five subtypes: D1, D2, D3, D4, and D5. The D1 and D5 subtypes are members of the D1-like family of dopamine receptors, whereas the D2, D3 and D4 subtypes are members of the D2-like family. The D1-like family receptors are coupled to G proteins of the G(s) family, which activate adenylate cyclase, causing cAMP formation and activation of protein kinase A. Dopamine receptors are major therapeutic targets for neurological and psychiatric disorders such as drug abuse, depression, schizophrenia, or Parkinson's disease. Pssm-ID: 320442 [Multi-domain] Cd Length: 317 Bit Score: 46.87 E-value: 8.91e-06
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| 7tmA_P2Y2 | cd15373 | P2Y purinoceptor 2, member of the class A family of seven-transmembrane G protein-coupled ... |
107-323 | 9.65e-06 | |||||
P2Y purinoceptor 2, member of the class A family of seven-transmembrane G protein-coupled receptors; P2Y2 belongs to the P2Y receptor family of purinergic G-protein coupled receptors and is implicated to play a role in the control of the cell cycle of endometrial carcinoma cells. The P2Y receptor family is composed of eight subtypes, which are activated by naturally occurring extracellular nucleotides such as ATP, ADP, UTP, UDP, and UDP-glucose. These eight receptors are ubiquitous in human tissues and can be further classified into two subfamilies based on sequence homology and second messenger coupling: a subfamily of five P2Y1-like receptors (P2Y1, P2Y2, P2Y4, P2Y6, and P2Y11Rs) that are coupled to G(q) protein to activate phospholipase C (PLC) and a second subfamily of three P2Y12-like receptors (P2Y12, P2YR13, and P2Y14Rs) that are coupled to G(i) protein to inhibit adenylate cyclase. Several cloned subtypes, such as P2Y3, P2Y5, and P2Y7-10, are not functional mammalian nucleotide receptors. The native agonists for P2Y receptors are: ATP (P2Y2, P2Y12), ADP (P2Y1, P2Y12, and P2Y13), UTP (P2Y2, P2Y4), UDP (P2Y6, P2Y14), and UDP-glucose (P2Y14). Pssm-ID: 320495 [Multi-domain] Cd Length: 283 Bit Score: 46.28 E-value: 9.65e-06
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| 7tmA_GPER1 | cd14989 | G protein-coupled estrogen receptor 1, member of the class A family of seven-transmembrane G ... |
75-325 | 1.02e-05 | |||||
G protein-coupled estrogen receptor 1, member of the class A family of seven-transmembrane G protein-coupled receptors; G-protein coupled estrogen receptor 1 (GPER1), also known as the G-protein coupled receptor 30 (GPR30), is a high affinity receptor for estrogen. This receptor is a member of the class A of seven-transmembrane GPCRs. Estrogen binding results in intracellular calcium mobilization and synthesis of phosphatidylinositol (3,4,5)-trisphosphate in the nucleus. GPR30 plays an important role in development of tamoxifen resistance in breast cancer cells. The distribution of GPR30 is well established in the rodent, with high expression observed in the hypothalamus, pituitary gland, adrenal medulla, kidney medulla and developing follicles of the ovary. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320120 [Multi-domain] Cd Length: 276 Bit Score: 46.36 E-value: 1.02e-05
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| PHA02834 | PHA02834 | chemokine receptor-like protein; Provisional |
106-283 | 1.14e-05 | |||||
chemokine receptor-like protein; Provisional Pssm-ID: 165177 Cd Length: 323 Bit Score: 46.44 E-value: 1.14e-05
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| 7tmA_CCR8 | cd15187 | CC chemokine receptor type 8, member of the class A family of seven-transmembrane G ... |
106-286 | 1.14e-05 | |||||
CC chemokine receptor type 8, member of the class A family of seven-transmembrane G protein-coupled receptors; CCR8, the receptor for the CC chemokines CCL1 and CC16, is highly expressed on allergen-specific T-helper type 2 cells, and is implicated in the pathogenesis of human asthma. CCL1- and CCR8-expressing CD4+ effector T lymphocytes are shown to have a critical role in lung mucosal inflammatory responses. CCR8 is also a functional receptor for CCL16, a liver-expressed CC chemokine that involved in attracting lymphocytes, dendritic cells, and monocytes. Chemokines are principal regulators for leukocyte trafficking, recruitment, and activation. Chemokine family membership is defined on the basis of sequence homology and on the presence of variations on a conserved cysteine motif, which allows the family to further divide into four subfamilies (CC, CXC, XC, and CX3C). Chemokines interact with seven-transmembrane receptors which are typically coupled to G protein for signaling. Currently, there are ten known receptors for CC chemokines, seven for CXC chemokines, and single receptors for the XC and CX3C chemokines. Pssm-ID: 320315 [Multi-domain] Cd Length: 276 Bit Score: 46.33 E-value: 1.14e-05
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| 7tmA_NMU-R2 | cd15357 | neuromedin U receptor subtype 2, member of the class A family of seven-transmembrane G ... |
83-327 | 1.18e-05 | |||||
neuromedin U receptor subtype 2, member of the class A family of seven-transmembrane G protein-coupled receptors; Neuromedin U (NMU) is a highly conserved neuropeptide with a common C-terminal heptapeptide sequence (FLFRPRN-amide) found at the highest levels in the gastrointestinal tract and pituitary gland of mammals. Disruption or replacement of residues in the conserved heptapeptide region can result in the reduced ability of NMU to stimulate smooth-muscle contraction. Two G-protein coupled receptor subtypes, NMU-R1 and NMU-R2, with a distinct expression pattern, have been identified to bind NMU. NMU-R1 is expressed primarily in the peripheral nervous system, while NMU-R2 is mainly found in the central nervous system. Neuromedin S, a 36 amino-acid neuropeptide that shares a conserved C-terminal heptapeptide sequence with NMU, is a highly potent and selective NMU-R2 agonist. Pharmacological studies have shown that both NMU and NMS inhibit food intake and reduce body weight, and that NMU increases energy expenditure. Pssm-ID: 320479 [Multi-domain] Cd Length: 293 Bit Score: 46.39 E-value: 1.18e-05
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| 7tmA_alpha1D_AR | cd15327 | alpha-1 adrenergic receptors subtype D, member of the class A family of seven-transmembrane G ... |
82-323 | 1.18e-05 | |||||
alpha-1 adrenergic receptors subtype D, member of the class A family of seven-transmembrane G protein-coupled receptors; The alpha-1 adrenergic receptors (or adrenoceptors) are a subfamily of the class A rhodopsin-like GPCRs that share a common architecture of seven transmembrane helices. This subfamily consists of three highly homologous receptor subtypes that primarily mediate smooth muscle contraction: alpha-1A, alpha-1B, and alpha-1D. Activation of alpha-1 receptors by catecholamines such as norepinephrine and epinephrine couples to the G(q) protein, which then activates the phospholipase C pathway, leading to an increase in IP3 and calcium. Consequently, the elevation of intracellular calcium concentration leads to vasoconstriction in smooth muscle of blood vessels. In addition, activation of alpha-1 receptors by phenylpropanolamine (PPA) produces anorexia and may induce appetite suppression in rats. Pssm-ID: 320450 [Multi-domain] Cd Length: 261 Bit Score: 46.06 E-value: 1.18e-05
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| 7tmA_GPR15 | cd15194 | G protein-coupled receptor 15, member of the class A family of seven-transmembrane G ... |
107-326 | 1.44e-05 | |||||
G protein-coupled receptor 15, member of the class A family of seven-transmembrane G protein-coupled receptors; GPR15, also called as Brother of Bonzo (BOB), is an orphan G-protein coupled receptor that was originally identified as a co-receptor for human immunodeficiency virus. GPR15 is upregulated in patients with rheumatoid arthritis and shares high sequence homology with angiotensin II type AT1 and AT2 receptors; however, its endogenous ligand is unknown. GPR15 controls homing of T cells, especially FOXP3(+) regulatory T cells, to the large intestine mucosa and thereby mediates local immune homeostasis. Moreover, GRP15-deficient mice were shown to be prone to develop more severe large intestine inflammation. Pssm-ID: 320322 [Multi-domain] Cd Length: 281 Bit Score: 46.00 E-value: 1.44e-05
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| 7tmA_P2Y1 | cd15377 | P2Y purinoceptor 1, member of the class A family of seven-transmembrane G protein-coupled ... |
71-323 | 1.55e-05 | |||||
P2Y purinoceptor 1, member of the class A family of seven-transmembrane G protein-coupled receptors; P2Y1 belongs to the P2Y receptor family of purinergic G-protein coupled receptors. This family is composed of eight subtypes, which are activated by naturally occurring extracellular nucleotides such as ATP, ADP, UTP, UDP, and UDP-glucose. These eight receptors are ubiquitous in human tissues and can be further classified into two subfamilies based on sequence homology and second messenger coupling: a subfamily of five P2Y1-like receptors (P2Y1, P2Y2, P2Y4, P2Y6, and P2Y11Rs) that are coupled to G(q) protein to activate phospholipase C (PLC) and a second subfamily of three P2Y12-like receptors (P2Y12, P2YR13, and P2Y14Rs) that are coupled to G(i) protein to inhibit adenylate cyclase. Several cloned subtypes, such as P2Y3, P2Y5, and P2Y7-10, are not functional mammalian nucleotide receptors. The native agonists for P2Y receptors are: ATP (P2Y2, P2Y12), ADP (P2Y1, P2Y12, and P2Y13), UTP (P2Y2, P2Y4), UDP (P2Y6, P2Y14), and UDP-glucose (P2Y14). Pssm-ID: 341350 [Multi-domain] Cd Length: 289 Bit Score: 45.67 E-value: 1.55e-05
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| 7tmA_CCR6 | cd15172 | CC chemokine receptor type 6, member of the class A family of seven-transmembrane G ... |
106-325 | 1.60e-05 | |||||
CC chemokine receptor type 6, member of the class A family of seven-transmembrane G protein-coupled receptors; CCR6 is the only known receptor identified for the chemokine CCL20 (also known as macrophage inflammatory protein-3alpha, MIP-3alpha). CCR6 is expressed by all mature human B cells, effector memory T-cells, and dendritic cells found in the gut mucosal immune system. CCL20 contributes to recruitment of CCR6-expressing cells to Peyer's patches and isolated lymphoid follicles in the intestine, thereby promoting the assembly and maintenance of organized lymphoid structures. Also, CCL20 expression is highly inducible in response to inflammatory signals. Thus, CCL20 is involved in both inflammatory and homeostatic functions in the immune system. Chemokines are principal regulators for leukocyte trafficking, recruitment, and activation. Chemokine family membership is defined on the basis of sequence homology and on the presence of variations on a conserved cysteine motif, which allows the family to further divide into four subfamilies (CC, CXC, XC, and CX3C). Chemokines interact with seven-transmembrane receptors which are typically coupled to G protein for signaling. Currently, there are ten known receptors for CC chemokines, seven for CXC chemokines, and single receptors for the XC and CX3C chemokines. The CC chemokine receptors are all activating the G protein Gi. Pssm-ID: 341330 [Multi-domain] Cd Length: 281 Bit Score: 45.90 E-value: 1.60e-05
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| 7tmA_SUCNR1_GPR91 | cd15378 | succinate receptor 1, member of the class A family of seven-transmembrane G protein-coupled ... |
106-286 | 1.75e-05 | |||||
succinate receptor 1, member of the class A family of seven-transmembrane G protein-coupled receptors; Succinate receptor (SUCNR1) GPR91 exclusively couples to G(i) protein to inhibit cAMP production and also activates PLC-beta to increase intracellular calcium concentrations in an inositol phosphate dependent mechanism. Succinate, an intermediate molecule of the citric cycle, is shown to cause cardiac hypertrophy via GPR91 activation. Furthermore, succinate-induced GPR91 activation is involved in the regulation of renin-angiotensin system and is suggested to play an important role in the development of renovascular hypertension and diabetic nephropathy. SUCNR1 belongs to the class A GPCR superfamily and is phylogenetically related to the purinergic P2Y1-like receptor subfamily, whose members are coupled to G(q) protein to activate phospholipase C (PLC). Pssm-ID: 320500 [Multi-domain] Cd Length: 283 Bit Score: 45.48 E-value: 1.75e-05
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| 7tmA_ET-BR | cd15976 | endothelin B receptor, member of the class A family of seven-transmembrane G protein-coupled ... |
78-321 | 1.88e-05 | |||||
endothelin B receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; Endothelins are able to activate a number of signal transduction processes including phospholipase A2, phospholipase C, and phospholipase D, as well as cytosolic protein kinase activation. They play an important role in the regulation of the cardiovascular system and are the most potent vasoconstrictors identified, stimulating cardiac contraction, regulating the release of vasoactive substances, and stimulating mitogenesis in blood vessels. Two endothelin receptor subtypes have been isolated and identified in vertebrates, endothelin A receptor (ET-A) and endothelin B receptor (ET-B), and are members of the seven transmembrane class A G-protein coupled receptor family which activate multiple effectors via different types of G protein. Some vertebrates contain a third subtype, endothelin A receptor (ET-C). ET-A receptors are mainly located on vascular smooth muscle cells, whereas ET-B receptors are present on endothelial cells lining the vessel wall. Endothelin receptors have also been found in the brain. Pssm-ID: 320642 [Multi-domain] Cd Length: 296 Bit Score: 45.62 E-value: 1.88e-05
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| 7tmA_Adenosine_R_A2A | cd15068 | adenosine receptor subtype A2A, member of the class A family of seven-transmembrane G ... |
130-325 | 1.91e-05 | |||||
adenosine receptor subtype A2A, member of the class A family of seven-transmembrane G protein-coupled receptors; The A2A receptor, a member of the adenosine receptor family of G protein-coupled receptors, binds adenosine as its endogenous ligand and is involved in regulating myocardial oxygen consumption and coronary blood flow. High-affinity A2A and low-affinity A2B receptors are preferentially coupled to G proteins of the stimulatory (Gs) family, which lead to activation of adenylate cyclase and thereby increasing the intracellular cAMP levels. The A2A receptor activation protects against tissue injury and acts as anti-inflammatory agent. In human skin endothelial cells, activation of A2B receptor, but not the A2A receptor, promotes angiogenesis. Alternatively, activated A2A receptor, but not the A2B receptor, promotes angiogenesis in human umbilical vein and lung microvascular endothelial cells. The A2A receptor alters cardiac contractility indirectly by modulating the anti-adrenergic effect of A1 receptor, while the A2B receptor exerts direct effects on cardiac contractile function, but does not modulate beta-adrenergic or A1 anti-adrenergic effects. Pssm-ID: 320196 [Multi-domain] Cd Length: 293 Bit Score: 45.70 E-value: 1.91e-05
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| 7tmA_GPR87 | cd15969 | G protein-coupled receptor 87, member of the class A family of seven-transmembrane G ... |
78-325 | 1.98e-05 | |||||
G protein-coupled receptor 87, member of the class A family of seven-transmembrane G protein-coupled receptors; GPR87 acts as one of multiple receptors for lysophosphatidic acid (LPA). This orphan receptor has been shown to be over-expressed in several malignant tumors including lung squamous cell carcinoma and regulated by p53. GPR87 is phylogenetically closely related to the G(i) class of the P2Y family of purinergic G protein-coupled receptors. P2Y receptor family is composed of eight subtypes, which are activated by naturally occurring extracellular nucleotides such as ATP, ADP, UTP, UDP, and UDP-sugars. These eight receptors are ubiquitous in human tissues and can be further classified into two subfamilies based on sequence homology and second messenger coupling: a subfamily of five P2Y1-like receptors (P2Y1, P2Y2, P2Y4, P2Y6, and P2Y11Rs) that are coupled to G(q) protein to activate phospholipase C (PLC) and a second subfamily of three P2Y12-like receptors (P2Y12, P2YR13, and P2Y14Rs) that are coupled to G(i) protein to inhibit adenylate cyclase. Pssm-ID: 320635 [Multi-domain] Cd Length: 283 Bit Score: 45.55 E-value: 1.98e-05
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| 7tmA_GPR132_G2A | cd15364 | proton-sensing G protein-coupled receptor 132, member of the class A family of ... |
100-286 | 1.99e-05 | |||||
proton-sensing G protein-coupled receptor 132, member of the class A family of seven-transmembrane G protein-coupled receptors; The G2 accumulation receptor (G2A, also known as GPR132) is a member of the proton-sensing G-protein-coupled receptor (GPCR) family which also includes the T cell death associated gene-8 (TDAG8, GPR65) receptor, ovarian cancer G-protein receptor 1 (OGR-1, GPR68), and G-protein-coupled receptor 4 (GPR4). Proton-sensing G-protein coupled receptors sense pH of 7.6 to 6.0 and mediates a variety of biological activities in neutral and mildly acidic pH conditions, whereas the acid-sensing ionotropic ion channels typically sense strong acidic pH. G2A was originally identified as a stress-inducible receptor that causes the cell cycle arrest at G2/M phase when serum is deprived. Lysophosphatidylcholine was identified as a ligand for G2A, and whose overexpression was shown to induce cell proliferation, oncogenic transformation, and apoptosis. Pssm-ID: 320486 [Multi-domain] Cd Length: 279 Bit Score: 45.54 E-value: 1.99e-05
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| 7tmA_Beta2_AR | cd15957 | beta-2 adrenergic receptors (adrenoceptors), member of the class A family of ... |
83-323 | 2.26e-05 | |||||
beta-2 adrenergic receptors (adrenoceptors), member of the class A family of seven-transmembrane G protein-coupled receptors; Beta-2 AR is activated by adrenaline that plays important roles in cardiac function and pulmonary physiology. While beta-1 AR and beta-2 AR are the major subtypes involved in modulating cardiac contractility and heart rate by positively stimulating the G(s) protein-adenylate cyclase-cAMP-PKA signaling pathway, beta-2 AR can couple to both G(s) and G(i) proteins in the heart. Moreover, beta-2 AR activation leads to smooth muscle relaxation and bronchodilation in the lung. The beta adrenergic receptors are a subfamily of the class A rhodopsin-like G protein-coupled receptors. Pssm-ID: 341355 [Multi-domain] Cd Length: 301 Bit Score: 45.24 E-value: 2.26e-05
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| 7tmA_D1A_dopamine_R | cd15320 | D1A (or D1) subtype dopamine receptor, member of the class A family of seven-transmembrane G ... |
83-325 | 2.46e-05 | |||||
D1A (or D1) subtype dopamine receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; Dopamine receptors are members of the class A G protein-coupled receptors that are involved in many neurological processes in the central nervous system (CNS). The neurotransmitter dopamine is the primary endogenous agonist for dopamine receptors. Dopamine receptors consist of at least five subtypes: D1, D2, D3, D4, and D5. The D1 and D5 subtypes are members of the D1-like family of dopamine receptors, whereas the D2, D3 and D4 subtypes are members of the D2-like family. The D1-like family receptors are coupled to G proteins of the G(s) family, which activate adenylate cyclase, causing cAMP formation and activation of protein kinase A. Dopamine receptors are major therapeutic targets for neurological and psychiatric disorders such as drug abuse, depression, schizophrenia, or Parkinson's disease. Pssm-ID: 320443 [Multi-domain] Cd Length: 319 Bit Score: 45.38 E-value: 2.46e-05
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| 7tmA_EDG-like | cd14972 | endothelial differentiation gene family, member of the class A family of seven-transmembrane G ... |
124-325 | 2.86e-05 | |||||
endothelial differentiation gene family, member of the class A family of seven-transmembrane G protein-coupled receptors; This group represents the endothelial differentiation gene (Edg) family of G-protein coupled receptors, melanocortin/ACTH receptors, and cannabinoid receptors as well as their closely related receptors. The Edg GPCRs bind blood borne lysophospholipids including sphingosine-1-phosphate (S1P) and lysophosphatidic acid (LPA), which are involved in the regulation of cell proliferation, survival, migration, invasion, endothelial cell shape change and cytoskeletal remodeling. The Edg receptors are classified into two subfamilies: the lysophosphatidic acid subfamily that includes LPA1 (Edg2), LPA2 (Edg4), and LPA3 (Edg7); and the S1P subfamily that includes S1P1 (Edg1), S1P2 (Edg5), S1P3 (Edg3), S1P4 (Edg6), and S1P5 (Edg8). Melanocortin receptors bind a group of pituitary peptide hormones known as melanocortins, which include adrenocorticotropic hormone (ACTH) and the different isoforms of melanocyte-stimulating hormones. Two types of cannabinoid receptors, CB1 and CB2, are activated by naturally occurring endocannabinoids, cannabis plant-derived cannabinoids such as tetrahydrocannabinol, or synthetic cannabinoids. The CB receptors are involved in the various physiological processes such as appetite, mood, memory, and pain sensation. CB1 receptor is expressed predominantly in central and peripheral neurons, while CB2 receptor is found mainly in the immune system. Pssm-ID: 341317 [Multi-domain] Cd Length: 275 Bit Score: 44.98 E-value: 2.86e-05
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| 7tmA_CCR5_CCR2 | cd15184 | CC chemokine receptor types 5 and 2, member of the class A family of seven-transmembrane G ... |
106-240 | 4.32e-05 | |||||
CC chemokine receptor types 5 and 2, member of the class A family of seven-transmembrane G protein-coupled receptors; CCR2 and CCR5 share very high amino acid sequence identity. Both receptors play important roles in the trafficking of monocytes/macrophages and are implicated in the pathogenesis of immunologic diseases (rheumatoid arthritis, celiac disease, and transplant rejection) and cardiovascular diseases (atherosclerosis and autoimmune hepatitis). CCR2 is a receptor specific for members of the monocyte chemotactic protein family, including CCL2, CCL7, and CCL13. Conversely, CCR5 is a major co-receptor for HIV infection and binds many CC chemokine ligands, including CC chemokine ligands including CCL2, CCL3, CCL4, CCL5, CCL11, CCL13, CCL14, and CCL16. CCR2 is expressed primarily on blood monocytes and memory T cells, whereas CCR5 is expressed on antigen-presenting cells (macrophages and dendritic cells) and activated T effector cells. Chemokines are principal regulators for leukocyte trafficking, recruitment, and activation. Chemokine family membership is defined on the basis of sequence homology and on the presence of variations on a conserved cysteine motif, which allows the family to further divide into four subfamilies (CC, CXC, XC, and CX3C). Chemokines interact with seven-transmembrane receptors which are typically coupled to G protein for signaling. Currently, there are ten known receptors for CC chemokines, seven for CXC chemokines, and single receptors for the XC and CX3C chemokines. Pssm-ID: 341338 [Multi-domain] Cd Length: 278 Bit Score: 44.36 E-value: 4.32e-05
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| 7tmA_RNL3R | cd14976 | relaxin-3 like peptide receptors, member of the class A family of seven-transmembrane G ... |
107-323 | 4.52e-05 | |||||
relaxin-3 like peptide receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; This G protein-coupled receptor subfamily is composed of the relaxin-3 like peptide receptors, RNL3R1 and RNL3R2, and similar proteins. The relaxin-3 like peptide family includes relaxin-1, -2, -3, as well as insulin-like (INSL) peptides 3 to 6. RNL3/relaxin-3 and INSL5 are the endogenous ligands for RNL3R1 and RNL3R2, respectively. RNL3R1, also called GPCR135 or RXFP3, is predominantly expressed in the brain and is implicated in stress, anxiety, feeding, and metabolism. Insulin-like peptide 5 (INSL5), the endogenous ligand for RNL3R2 (also called GPCR142 or RXFP4), plays a role in fat and glucose metabolism. INSL5 is highly expressed in human rectal and colon tissues. Both RNL3R1 and RNL3R2 signal through G(i) protein and inhibit adenylate cyclase, thereby inhibit cAMP accumulation. RNL3R1 is shown to activate Erk1/2 signaling pathway. Pssm-ID: 320107 [Multi-domain] Cd Length: 290 Bit Score: 44.42 E-value: 4.52e-05
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| 7tmA_mAChR_M5 | cd15300 | muscarinic acetylcholine receptor subtype M5, member of the class A family of ... |
80-324 | 4.74e-05 | |||||
muscarinic acetylcholine receptor subtype M5, member of the class A family of seven-transmembrane G protein-coupled receptors; Muscarinic acetylcholine receptors (mAChRs) regulate the activity of many fundamental central and peripheral functions. The mAChR family consists of 5 subtypes M1-M5, which can be further divided into two major groups according to their G-protein coupling preference. The M1, M3 and M5 receptors selectively interact with G proteins of the G(q/11) family, whereas the M2 and M4 receptors preferentially link to the G(i/o) types of G proteins. M5 mAChR is primarily found in the central nervous system and mediates acetylcholine-induced dilation of cerebral blood vessels. Activation of M5 receptor triggers a variety of cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides, and modulation of potassium channels. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320427 [Multi-domain] Cd Length: 262 Bit Score: 44.25 E-value: 4.74e-05
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| 7tmA_NTSR2 | cd15356 | neurotensin receptor subtype 2, member of the class A family of seven-transmembrane G ... |
39-314 | 5.35e-05 | |||||
neurotensin receptor subtype 2, member of the class A family of seven-transmembrane G protein-coupled receptors; Neurotensin (NTS) is a 13 amino-acid neuropeptide that functions as both a neurotransmitter and a hormone in the nervous system and peripheral tissues, respectively. NTS exerts various biological activities through activation of the G protein-coupled neurotensin receptors, NTSR1 and NTSR2. In the brain, NTS is involved in the modulation of dopamine neurotransmission, opioid-independent analgesia, hypothermia, and the inhibition of food intake, while in the periphery NTS promotes the growth of various normal and cancer cells and acts as a paracrine and endocrine modulator of the digestive tract. The third neurotensin receptor, NTSR3 or also called sortilin, is not a G protein-coupled receptor. Pssm-ID: 320478 [Multi-domain] Cd Length: 285 Bit Score: 44.09 E-value: 5.35e-05
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| 7tmA_BK-2 | cd15381 | bradykinin receptor B2, member of the class A family of seven-transmembrane G protein-coupled ... |
101-323 | 5.35e-05 | |||||
bradykinin receptor B2, member of the class A family of seven-transmembrane G protein-coupled receptors; The bradykinin receptor family is a group of the seven transmembrane G-protein coupled receptors, whose endogenous ligand is the pro-inflammatory nonapeptide bradykinin that mediates various vascular and pain responses. Two major bradykinin receptor subtypes, B1 and B2, have been identified based on their pharmacological properties. The B1 receptor is rapidly induced by tissue injury and inflammation, whereas the B2 receptor is ubiquitously expressed on many tissue types. Both receptors contain three consensus sites for N-linked glycosylation in extracellular domains and couple to G(q) protein to activate phospholipase C, leading to phosphoinositide hydrolysis and intracellular calcium mobilization. They can also interact with G(i) protein to inhibit adenylate cyclase and activate the MAPK (mitogen-activated protein kinase) pathways. Pssm-ID: 320503 [Multi-domain] Cd Length: 284 Bit Score: 43.99 E-value: 5.35e-05
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| 7tmA_CCR3 | cd15185 | CC chemokine receptor type 3, member of the class A family of seven-transmembrane G ... |
101-325 | 6.46e-05 | |||||
CC chemokine receptor type 3, member of the class A family of seven-transmembrane G protein-coupled receptors; CCR3 is a highly promiscuous receptor that binds a variety of inflammatory CC-type chemokines, including CCL11 (eotaxin-1), CCL3L1, CCL5 (regulated on activation, normal T cell expressed and secreted; RANTES), CCL7 (monocyte-specific chemokine 3 or MCP-3), CCL8 (MCP-2), CCL11, CCL13 (MCP-4), CCL15, CCL24 (eotaxin-2), CCL26 (eotaxin-3), and CCL28. Among these, the eosinophil chemotactic chemokines (CCL11, CCL24, and CCL26) are the most potent and specific ligands. In addition to eosinophil, CCR3 is expressed on cells involved in allergic responses, such as basophils, Th2 lymphocytes, and mast cells. Chemokines are principal regulators for leukocyte trafficking, recruitment, and activation. Chemokine family membership is defined on the basis of sequence homology and on the presence of variations on a conserved cysteine motif, which allows the family to further divide into four subfamilies (CC, CXC, XC, and CX3C). Chemokines interact with seven-transmembrane receptors which are typically coupled to G protein for signaling. Currently, there are ten known receptors for CC chemokines, seven for CXC chemokines, and single receptors for the XC and CX3C chemokines. Pssm-ID: 341339 [Multi-domain] Cd Length: 278 Bit Score: 44.05 E-value: 6.46e-05
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| 7tmA_Parapinopsin | cd15075 | non-visual parapinopsin, member of the class A family of seven-transmembrane G protein-coupled ... |
134-296 | 6.65e-05 | |||||
non-visual parapinopsin, member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes the non-visual pineal pigment, parapinopsin, which is a member of the class A of the seven transmembrane G protein-coupled receptors. Parapinopsin serves as a UV-sensitive pigment for the wavelength discrimination in the pineal-related organs of lower vertebrates such as reptiles, amphibians, and fish. Although parapinopsin is phylogenetically related to vertebrate visual pigments such as rhodopsin, which releases its retinal chromophore and bleaches, the parapinopsin photoproduct is stable and does not bleach. The vertebrate non-visual opsin family includes pinopsins, parapinopsin, VA (vertebrate ancient) opsins, and parietopsins. These non-visual opsins are expressed in various extra-retinal tissues and/or in non-rod, non-cone retinal cells. Pssm-ID: 320203 [Multi-domain] Cd Length: 279 Bit Score: 44.00 E-value: 6.65e-05
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| 7tmA_SSTR5 | cd15974 | somatostatin receptor type 5, member of the class A family of seven-transmembrane G ... |
95-327 | 6.92e-05 | |||||
somatostatin receptor type 5, member of the class A family of seven-transmembrane G protein-coupled receptors; G protein-coupled somatostatin receptors (SSTRs) are composed of five distinct subtypes (SSTR1-5) that display strong sequence similarity with opioid receptors. All five receptor subtypes bind the natural somatostatin (somatotropin release inhibiting factor), a polypeptide hormone that regulates a wide variety of physiological functions such as neurotransmission, cell proliferation, contractility of smooth muscle cells, and endocrine signaling as well as inhibition of the release of many secondary hormones. SSTR5 is coupled to inward rectifying K channels and phospholipase C, and plays critical roles in growth hormone and insulin secretion. SSTR5 acts as a negative regulator of PDX-1 (pancreatic and duodenal homeobox-1) expression, which is a conserved homeodomain-containing beta cell-specific transcription factor essentially involved in pancreatic development, among many other functions. Pssm-ID: 320640 [Multi-domain] Cd Length: 277 Bit Score: 43.64 E-value: 6.92e-05
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| 7tmA_SWS2_opsin | cd15077 | short wave-sensitive 2 opsins, member of the class A family of seven-transmembrane G ... |
43-289 | 7.12e-05 | |||||
short wave-sensitive 2 opsins, member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes Short Wave-Sensitive opsin 2 (SWS2), which mediates visual transduction in response to light at short wavelengths (violet to blue). Vertebrate cone opsins are expressed in cone photoreceptor cells of the retina and involved in mediating photopic vision, which allows color perception. The cone opsins can be classified into four classes according to their peak absorption wavelengths: SWS1 (ultraviolet sensitive), SWS2 (short wave-sensitive), MWS/LWS (medium/long wave-sensitive), and RH2 (medium wave-sensitive, rhodopsin-like opsins). Members of this group belong to the class A of the G protein-coupled receptors and possess seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. Pssm-ID: 320205 [Multi-domain] Cd Length: 280 Bit Score: 43.66 E-value: 7.12e-05
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| 7tmA_LWS_opsin | cd15081 | long wave-sensitive opsins, member of the class A family of seven-transmembrane G ... |
69-294 | 8.14e-05 | |||||
long wave-sensitive opsins, member of the class A family of seven-transmembrane G protein-coupled receptors; Long Wave-Sensitive opsin is also called red-sensitive opsin or red cone photoreceptor pigment, which mediates visual transduction in response to light at long wavelengths. Vertebrate cone opsins are expressed in cone photoreceptor cells of the retina and involved in mediating photopic vision, which allows color perception. The cone opsins can be classified into four classes according to their peak absorption wavelengths: SWS1 (ultraviolet sensitive), SWS2 (short wave-sensitive), MWS/LWS (medium/long wave-sensitive), and RH2 (medium wave-sensitive, rhodopsin-like opsins). Members of this group belong to the class A of the G protein-coupled receptors and possess seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. Pssm-ID: 320209 [Multi-domain] Cd Length: 292 Bit Score: 43.74 E-value: 8.14e-05
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| 7tmA_D3_dopamine_R | cd15310 | D3 subtype of the D2-like family of dopamine receptors, member of the class A family of ... |
79-328 | 8.79e-05 | |||||
D3 subtype of the D2-like family of dopamine receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Dopamine receptors are members of the class A G protein-coupled receptors that are involved in many neurological processes in the central nervous system (CNS). The neurotransmitter dopamine is the primary endogenous agonist for dopamine receptors. Dopamine receptors consist of at least five subtypes: D1, D2, D3, D4, and D5. The D1 and D5 subtypes are members of the D1-like family of dopamine receptors, whereas the D2, D3 and D4 subtypes are members of the D2-like family. Activation of D2-like family receptors is linked to G proteins of the G(i) family. This leads to a decrease in adenylate cyclase activity, thereby decreasing cAMP levels. Dopamine receptors are major therapeutic targets for neurological and psychiatric disorders such as drug abuse, depression, schizophrenia, or Parkinson's disease. Pssm-ID: 320436 [Multi-domain] Cd Length: 259 Bit Score: 43.42 E-value: 8.79e-05
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| 7tmA_GPR26_GPR78-like | cd15219 | G protein-coupled receptors 26 and 78, member of the class A family of seven-transmembrane G ... |
78-285 | 1.15e-04 | |||||
G protein-coupled receptors 26 and 78, member of the class A family of seven-transmembrane G protein-coupled receptors; Orphan G-protein coupled receptor 26 (GPR26) and GPR78 are constitutively active and coupled to increased cAMP formation. They are closely related based on sequence homology and comprise a conserved subgroup within the class A G-protein coupled receptor (GPCR) superfamily. Both receptors are widely expressed in selected tissues of the brain but their endogenous ligands are unknown. GPR26 knockout mice showed increased levels of anxiety- and depression-like behaviors, whereas GPR78 has been implicated in susceptibility to bipolar affective disorder and schizophrenia. Members of this subgroup contain the highly conserved Asp-Arg-Tyr/Phe (DRY/F) motif found in the third transmembrane helix (TM3) of the rhodopsin-like class A receptors which is important for efficient G protein-coupled signal transduction. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320347 [Multi-domain] Cd Length: 264 Bit Score: 43.22 E-value: 1.15e-04
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| 7tmA_OXER1 | cd15200 | oxoeicosanoid receptor 1, member of the class A family of seven-transmembrane G ... |
107-327 | 1.21e-04 | |||||
oxoeicosanoid receptor 1, member of the class A family of seven-transmembrane G protein-coupled receptors; OXER1, also called GPR170, is a receptor for eicosanoids and polyunsaturated fatty acids such as 5-oxo-6E,8Z,11Z,14Z-eicosatetraenoic acid (5-OXO-ETE), 5(S)-hydroperoxy-6E,8Z,11Z,14Z-eicosatetraenoic acid (5(S)-HPETE) and arachidonic acid. OXER1 is a member of the class A family of seven-transmembrane G-protein coupled receptors and appears to be coupled to the G(i/o) protein. The receptor is expressed in various tissues except brain. Phylogenetic analysis showed that GPR31 and OXER1 are the most closely related receptors to the hydroxycarboxylic acid receptor family (HCARs). OXER1, like GPR31, activates the ERK1/2 (MAPK3/MAPK1) pathway of intracellular signaling, but unlike GPR31, does cause increase in the cytosolic calcium level. Pssm-ID: 320328 [Multi-domain] Cd Length: 276 Bit Score: 43.22 E-value: 1.21e-04
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| 7tmA_P2Y4 | cd15374 | P2Y purinoceptor 4, member of the class A family of seven-transmembrane G protein-coupled ... |
82-323 | 1.25e-04 | |||||
P2Y purinoceptor 4, member of the class A family of seven-transmembrane G protein-coupled receptors; P2Y4 belongs to the P2Y receptor family of purinergic G-protein coupled receptors. This family is composed of eight subtypes, which are activated by naturally occurring extracellular nucleotides such as ATP, ADP, UTP, UDP, and UDP-glucose. These eight receptors are ubiquitous in human tissues and can be further classified into two subfamilies based on sequence homology and second messenger coupling: a subfamily of five P2Y1-like receptors (P2Y1, P2Y2, P2Y4, P2Y6, and P2Y11Rs) that are coupled to G(q) protein to activate phospholipase C (PLC) and a second subfamily of three P2Y12-like receptors (P2Y12, P2YR13, and P2Y14Rs) that are coupled to G(i) protein to inhibit adenylate cyclase. Several cloned subtypes, such as P2Y3, P2Y5, and P2Y7-10, are not functional mammalian nucleotide receptors. The native agonists for P2Y receptors are: ATP (P2Y2, P2Y12), ADP (P2Y1, P2Y12, and P2Y13), UTP (P2Y2, P2Y4), UDP (P2Y6, P2Y14), and UDP-glucose (P2Y14). Pssm-ID: 320496 [Multi-domain] Cd Length: 285 Bit Score: 42.87 E-value: 1.25e-04
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| 7tmA_Mel1B | cd15400 | melatonin receptor subtype 1B, member of the class A family of seven-transmembrane G ... |
83-324 | 1.45e-04 | |||||
melatonin receptor subtype 1B, member of the class A family of seven-transmembrane G protein-coupled receptors; Melatonin (N-acetyl-5-methoxytryptamine) is a naturally occurring sleep-promoting chemical found in vertebrates, invertebrates, bacteria, fungi, and plants. In mammals, melatonin is secreted by the pineal gland and is involved in regulation of circadian rhythms. Its production peaks during the nighttime, and is suppressed by light. Melatonin is shown to be synthesized in other organs and cells of many vertebrates, including the Harderian gland, leukocytes, skin, and the gastrointestinal (GI) tract, which contains several hundred times more melatonin than the pineal gland and is involved in the regulation of GI motility, inflammation, and sensation. Melatonin exerts its pleiotropic physiological effects through specific membrane receptors, named MT1A, MT1B, and MT1C, which belong to the class A rhodopsin-like G-protein coupled receptor family. MT1A and MT1B subtypes are present in mammals, whereas MT1C subtype has been found in amphibians and birds. The melatonin receptors couple to G proteins of the G(i/o) class, leading to the inhibition of adenylate cyclase. Pssm-ID: 320522 [Multi-domain] Cd Length: 279 Bit Score: 42.92 E-value: 1.45e-04
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| 7tmA_mAChR_M4 | cd15298 | muscarinic acetylcholine receptor subtype M4, member of the class A family of ... |
79-286 | 1.52e-04 | |||||
muscarinic acetylcholine receptor subtype M4, member of the class A family of seven-transmembrane G protein-coupled receptors; Muscarinic acetylcholine receptors (mAChRs) regulate the activity of many fundamental central and peripheral functions. The mAChR family consists of 5 subtypes M1-M5, which can be further divided into two major groups according to their G-protein coupling preference. The M1, M3 and M5 receptors selectively interact with G proteins of the G(q/11) family, whereas the M2 and M4 receptors preferentially link to G(i/o) types of G proteins. The M4 receptor is mainly found in the CNS and function as an inhibitory autoreceptor regulating acetycholine release. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 341344 [Multi-domain] Cd Length: 262 Bit Score: 42.70 E-value: 1.52e-04
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| 7tmA_Adenosine_R | cd14968 | adenosine receptor subfamily, member of the class A family of seven-transmembrane G ... |
83-325 | 1.67e-04 | |||||
adenosine receptor subfamily, member of the class A family of seven-transmembrane G protein-coupled receptors; The adenosine receptors (or P1 receptors), a family of G protein-coupled purinergic receptors, bind adenosine as their endogenous ligand. There are four types of adenosine receptors in human, designated as A1, A2A, A2B, and A3. Each type is encoded by a different gene and has distinct functions with some overlap. For example, both A1 and A2A receptors are involved in regulating myocardial oxygen consumption and coronary blood flow in the heart, while the A2A receptor also has a broad spectrum of anti-inflammatory effects in the body. These two receptors also expressed in the brain, where they have important roles in the release of other neurotransmitters such as dopamine and glutamate, while the A2B and A3 receptors found primarily in the periphery and play important roles in inflammation and immune responses. The A1 and A3 receptors preferentially interact with G proteins of the G(i/o) family, thereby lowering the intracellular cAMP levels, whereas the A2A and A2B receptors interact with G proteins of the G(s) family, activating adenylate cyclase to elevate cAMP levels. Pssm-ID: 341316 [Multi-domain] Cd Length: 285 Bit Score: 42.63 E-value: 1.67e-04
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| 7tmA_CCR7 | cd15175 | CC chemokine receptor type 7, member of the class A family of seven-transmembrane G ... |
71-238 | 1.81e-04 | |||||
CC chemokine receptor type 7, member of the class A family of seven-transmembrane G protein-coupled receptors; CCR7 is a major homeostatic receptor responsible for lymph node development and effective adaptive immune responses and plays a critical role in trafficking of dendritic cells and B and T lymphocytes. Its only two ligands, CCL and CCl21, are primarily produced by stromal cells in the T cell zones of lymph nodes and spleen. Chemokines are principal regulators for leukocyte trafficking, recruitment, and activation. Chemokine family membership is defined on the basis of sequence homology and on the presence of variations on a conserved cysteine motif, which allows the family to further divide into four subfamilies (CC, CXC, XC, and CX3C). Chemokines interact with seven-transmembrane receptors which are typically coupled to G protein for signaling. Currently, there are ten known receptors for CC chemokines, seven for CXC chemokines, and single receptors for the XC and CX3C chemokines. The CC chemokine receptors are all activating the G protein Gi. Pssm-ID: 341331 [Multi-domain] Cd Length: 278 Bit Score: 42.44 E-value: 1.81e-04
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| 7tmA_Glycoprotein_LRR_R-like | cd14980 | glycoprotein hormone receptors and leucine-rich repeats containing G protein-coupled receptors, ... |
113-327 | 1.90e-04 | |||||
glycoprotein hormone receptors and leucine-rich repeats containing G protein-coupled receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; This subfamily includes the glycoprotein hormone receptors (GPHRs), vertebrate receptors containing 17 leucine-rich repeats (LGR4-6), and the relaxin family peptide receptors (also known as LGR7 and LGR8). They are seven transmembrane domain receptors with a very large extracellular N-terminal domain containing many leucine-rich repeats responsible for hormone recognition and binding. The glycoprotein hormone receptor family contains receptors for the pituitary hormones, thyrotropin (thyroid-stimulating hormone receptor), follitropin (follicle-stimulating hormone receptor), and lutropin (luteinizing hormone receptor). Glycoprotein hormone receptors couple primarily to the G(s)-protein and promotes cAMP production, but also to the G(i)- or G(q)-protein. Two orphan GPCRs, LGR7 and LGR8, have been recently identified as receptors for the relaxin peptide hormones. Pssm-ID: 320111 [Multi-domain] Cd Length: 286 Bit Score: 42.61 E-value: 1.90e-04
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| 7tmA_RNL3R1 | cd15926 | relaxin 3 receptor 1 (RNL3R1), member of the class A family of seven-transmembrane G ... |
66-289 | 2.16e-04 | |||||
relaxin 3 receptor 1 (RNL3R1), member of the class A family of seven-transmembrane G protein-coupled receptors; The G protein-coupled receptor RNL3R1 is also known as GPCR135, relaxin family peptide receptor 3 (RXFP3), and somatostatin- and angiotensin-like peptide receptor (SALPR). RNL3/relaxin-3, a member of the insulin superfamily, is an endogenous neuropeptide ligand for RNL3R1. RNL3R1 is predominantly expressed in brain regions and implicated in stress, anxiety, and feeding, and metabolism. RNL3R1 signals through G(i) protein and inhibit adenylate cyclase, thereby inhibit cAMP accumulation, and also activates Erk1/2 signaling pathway. Pssm-ID: 320592 [Multi-domain] Cd Length: 288 Bit Score: 42.19 E-value: 2.16e-04
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| 7tmA_NPY5R | cd15398 | neuropeptide Y receptor type 5, member of the class A family of seven-transmembrane G ... |
68-327 | 2.42e-04 | |||||
neuropeptide Y receptor type 5, member of the class A family of seven-transmembrane G protein-coupled receptors; NPY is a 36-amino acid peptide neurotransmitter with a C-terminal tyrosine amide residue that is widely distributed in the brain and the autonomic nervous system of many mammalian species. NPY exerts its functions through five, G-protein coupled receptor subtypes including NPY1R, NPY2R, NPY4R, NPY5R, and NPY6R; however, NPY6R is not functional in humans. NYP receptors are also activated by its two other family members, peptide YY (PYY) and pancreatic polypeptide (PP). They typically couple to G(i) or G(o) proteins, which leads to a decrease in adenylate cyclase activity, thereby decreasing intracellular cAMP levels, and are involved in diverse physiological roles including appetite regulation, circadian rhythm, and anxiety. When NPY signals through NPY2R in concert with NPY5R, it induces angiogenesis and consequently plays an important role in revascularization and wound healing. On the other hand, when NPY acts through NPY1R and NPYR5, it acts as a vascular mitogen, leading to restenosis and atherosclerosis. Pssm-ID: 320520 [Multi-domain] Cd Length: 273 Bit Score: 42.06 E-value: 2.42e-04
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| 7tmA_GPR31 | cd15199 | G protein-coupled receptor 31, member of the class A family of seven-transmembrane G ... |
80-323 | 2.86e-04 | |||||
G protein-coupled receptor 31, member of the class A family of seven-transmembrane G protein-coupled receptors; GPR31, also known as 12-(S)-HETE receptor, is a high-affinity receptor for 12-(S)-hydroxy-5,8,10,14-eicosatetraenoic acid. Phylogenetic analysis showed that GPR31 and oxoeicosanoid receptor 1 (OXER1, GPR170) are the most closely related receptors to the hydroxycarboxylic acid receptor family (HCARs). GPR31, like OXER1, activates the ERK1/2 (MAPK3/MAPK1) pathway of intracellular signaling, but unlike the OXER1, does not cause increase in the cytosolic calcium level. GPR31 is also shown to activate NFkB. 12-(S)-HETE is a 12-lipoxygenase metabolite of arachidonic acid produced by mammalian platelets and tumor cells. It promotes tumor cells adhesion to endothelial cells and sub-endothelial matrix, which is a critical step for metastasis. Pssm-ID: 320327 [Multi-domain] Cd Length: 278 Bit Score: 42.09 E-value: 2.86e-04
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| 7tmA_ACKR3_CXCR7 | cd14987 | CXC chemokine receptor 7, member of the class A family of seven-transmembrane G ... |
106-325 | 3.11e-04 | |||||
CXC chemokine receptor 7, member of the class A family of seven-transmembrane G protein-coupled receptors; ACKR3, also known as CXCR7, is an atypical chemokine receptor for CXCL12 and CXCR11. Unlike the classical chemokine receptors, ACKR3 contains a DRYLSIT-sequence instead of the conserved DRYLAIV motif in the second intracellular loop, which is required for G-protein coupling. Thus, ACKR3 does not activate classical GPCR signaling, instead induces beta-arrestin recruitment which is leading to ligand internalization and MAP-kinase activation. It is acting as a scavenger for CXCL12 and, to a lesser degree, for CXCL11. ACKR3 is highly expressed by blood vascular endothelial cells in brain, in numerous embryonic and neonatal tissues, in inflamed tissues and in a variety of cancers such as lymphomas, sarcomas, prostate and breast cancers, and gliomas. Five receptors have been identified for the ACKR family, including CC-Chemokine Receptors like 1 and 2 (CCRL1 and CCRL2), CXCR7, DARC, and D6. Both ACKR1 (DARC) and ACKR3 (CXCR7) show low sequence homology to the classic chemokine receptors. Pssm-ID: 320118 [Multi-domain] Cd Length: 282 Bit Score: 41.67 E-value: 3.11e-04
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| 7tmA_GPR68_OGR1 | cd15367 | G protein-coupled receptor 68, member of the class A family of seven-transmembrane G ... |
107-286 | 3.38e-04 | |||||
G protein-coupled receptor 68, member of the class A family of seven-transmembrane G protein-coupled receptors; The ovarian cancer G-protein receptor 1 (OGR1, also known as GPR68) is a member of the proton-sensing G-protein-coupled receptor (GPCR) family which also includes the G2 accumulation receptor (G2A, also known as GPR132), the T cell death associated gene-8 receptor (TDAG8, GPR65), and the G-protein-coupled receptor 4 (GPR4). Proton-sensing G-protein coupled receptors sense pH of 7.6 to 6.0 and mediates a variety of biological activities in neutral and mildly acidic pH conditions, whereas the acid-sensing ionotropic ion channels typically sense strong acidic pH. Knock-out mice studies have suggested that OGR1 plays a role in the regulation of insulin secretion and glucose metabolism. OGR1 couples to G(q/11) proteins and activates phospholipase C and Ca2+ signaling pathways. Pssm-ID: 320489 [Multi-domain] Cd Length: 276 Bit Score: 41.67 E-value: 3.38e-04
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| 7tmA_GPR135 | cd15212 | G protein-coupled receptor 135, member of the class A family of seven-transmembrane G ... |
83-288 | 3.57e-04 | |||||
G protein-coupled receptor 135, member of the class A family of seven-transmembrane G protein-coupled receptors; GPR135, also known as the somatostatin- and angiotensin-like peptide receptor (SALPR), is found in various tissues including eye, brain, cervix, stomach, and testis. Pharmacological studies have shown that relaxin-3 (R3) is a high-affinity endogenous ligand for GPR135. R3 has recently been identified as a new member of the insulin/relaxin family of peptide hormones and is exclusively expressed in the brain neurons. In addition to GPR135, R3 also acts as an agonist for GPR142, a pseudogene in the rat, and can activate LGR7 (leucine repeat-containing G-protein receptor-7), which is the main receptor for relaxin-1 (R1) and relaxin-2 (R2). While R1 and R2 are hormones primarily associated with reproduction and pregnancy, R3 is involved in neuroendocrine and sensory processing. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320340 [Multi-domain] Cd Length: 285 Bit Score: 41.68 E-value: 3.57e-04
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| 7tmA_CXCR6 | cd15173 | CXC chemokine receptor type 6, member of the class A family of seven-transmembrane G ... |
106-328 | 3.90e-04 | |||||
CXC chemokine receptor type 6, member of the class A family of seven-transmembrane G protein-coupled receptors; CXCR6 binds specifically to the chemokine CXCL16, which is expressed on dendritic cells, monocyte/macrophages, activated T cells, fibroblastic reticular cells, and cancer cells. CXCR6 is phylogenetically more closely related to CC-type chemokine receptors (CCR6 and CCR9) than other CXC receptors. Chemokines are principal regulators for leukocyte trafficking, recruitment, and activation. Chemokine family membership is defined on the basis of sequence homology and on the presence of variations on a conserved cysteine motif, which allows the family to further divide into four subfamilies (CC, CXC, XC, and CX3C). Chemokines interact with seven-transmembrane receptors which are typically coupled to G protein for signaling. Currently, there are ten known receptors for CC chemokines, seven for CXC chemokines, and single receptors for the XC and CX3C chemokines. Pssm-ID: 320301 [Multi-domain] Cd Length: 270 Bit Score: 41.29 E-value: 3.90e-04
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| 7tmA_Histamine_H4R | cd15295 | histamine receptor subtype H4R, member of the class A family of seven-transmembrane G ... |
75-323 | 4.06e-04 | |||||
histamine receptor subtype H4R, member of the class A family of seven-transmembrane G protein-coupled receptors; This group includes histamine subtype H4R, a member of the histamine receptor family, which belong to the class A of GPCRs. Histamine plays a key role as chemical mediator and neurotransmitter in various physiological and pathophysiological processes in the central and peripheral nervous system. Histamine exerts its functions by binding to four different G protein-coupled receptors (H1-H4). The H3 and H4 receptors couple to the G(i)-proteins, which leading to the inhibition of cAMP formation. The H3R receptor functions as a presynaptic autoreceptors controlling histamine release and synthesis. The H4R plays an important role in histamine-mediated chemotaxis in mast cells and eosinophils. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320422 [Multi-domain] Cd Length: 267 Bit Score: 41.35 E-value: 4.06e-04
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| 7tmA_P2Y11 | cd15376 | P2Y purinoceptor 11, member of the class A family of seven-transmembrane G protein-coupled ... |
83-324 | 4.20e-04 | |||||
P2Y purinoceptor 11, member of the class A family of seven-transmembrane G protein-coupled receptors; P2Y11 belongs to the P2Y receptor family of purinergic G-protein coupled receptors. The activation of P2Y11 is a major pathway of macrophage activation that leads to the release of cytokines. The P2Y receptor family is composed of eight subtypes, which are activated by naturally occurring extracellular nucleotides such as ATP, ADP, UTP, UDP, and UDP-glucose. These eight receptors are ubiquitous in human tissues and can be further classified into two subfamilies based on sequence homology and second messenger coupling: a subfamily of five P2Y1-like receptors (P2Y1, P2Y2, P2Y4, P2Y6, and P2Y11Rs) that are coupled to G(q) protein to activate phospholipase C (PLC) and a second subfamily of three P2Y12-like receptors (P2Y12, P2YR13, and P2Y14Rs) that are coupled to G(i) protein to inhibit adenylate cyclase. Several cloned subtypes, such as P2Y3, P2Y5, and P2Y7-10, are not functional mammalian nucleotide receptors. The native agonists for P2Y receptors are: ATP (P2Y2, P2Y12), ADP (P2Y1, P2Y12, and P2Y13), UTP (P2Y2, P2Y4), UDP (P2Y6, P2Y14), and UDP-glucose (P2Y14). Pssm-ID: 320498 [Multi-domain] Cd Length: 284 Bit Score: 41.22 E-value: 4.20e-04
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| 7tmA_GPR20 | cd15163 | G protein-coupled receptor 20, member of the class A family of seven-transmembrane G ... |
114-323 | 4.30e-04 | |||||
G protein-coupled receptor 20, member of the class A family of seven-transmembrane G protein-coupled receptors; Orphan GPR20 is phylogenetically related to the P2Y family of purinergic G protein-coupled receptors. The P2Y receptor family is composed of eight subtypes, which are activated by naturally occurring extracellular nucleotides such as ATP, ADP, UTP, UDP, and UDP-glucose. GPR20 has been shown to constitutively activate G(i) proteins in the absence of a ligand; however its functional role is not known. GPR20 is a member of the class A G protein-coupled receptor superfamily, which all have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A common feature of GPCR signaling is agonist-induced conformational changes in the receptors, which then activate the heterotrimeric G proteins. G-proteins regulate a variety of cellular functions including metabolic enzymes, ion channels, and transporters, among many others. Pssm-ID: 320291 [Multi-domain] Cd Length: 258 Bit Score: 41.32 E-value: 4.30e-04
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| 7tmA_Melanopsin | cd15336 | vertebrate melanopsins (Opsin-4), member of the class A family of seven-transmembrane G ... |
83-291 | 4.79e-04 | |||||
vertebrate melanopsins (Opsin-4), member of the class A family of seven-transmembrane G protein-coupled receptors; Melanopsin (also called Opsin-4) is the G protein-coupled photopigment that mediates non-visual responses to light. In mammals, these photoresponses include the photo-entrainment of circadian rhythm, pupillary constriction, and acute nocturnal melatonin suppression. Mammalian melanopsins are expressed only in the inner retina, whereas non-mammalian vertebrate melanopsins are localized in various extra-retinal tissues such as iris, brain, pineal gland, and skin. Melanopsins belong the class A of the G protein-coupled receptors and possess seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. Pssm-ID: 320458 [Multi-domain] Cd Length: 290 Bit Score: 41.24 E-value: 4.79e-04
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| 7tm_GPCRs | cd14964 | seven-transmembrane G protein-coupled receptor superfamily; This hierarchical evolutionary ... |
78-327 | 6.37e-04 | |||||
seven-transmembrane G protein-coupled receptor superfamily; This hierarchical evolutionary model represents the seven-transmembrane (7TM) receptors, often referred to as G protein-coupled receptors (GPCRs), which transmit physiological signals from the outside of the cell to the inside via G proteins. GPCRs constitute the largest known superfamily of transmembrane receptors across the three kingdoms of life that respond to a wide variety of extracellular stimuli including peptides, lipids, neurotransmitters, amino acids, hormones, and sensory stimuli such as light, smell and taste. All GPCRs share a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. However, some 7TM receptors, such as the type 1 microbial rhodopsins, do not activate G proteins. Based on sequence similarity, GPCRs can be divided into six major classes: class A (the rhodopsin-like family), class B (the Methuselah-like, adhesion and secretin-like receptor family), class C (the metabotropic glutamate receptor family), class D (the fungal mating pheromone receptors), class E (the cAMP receptor family), and class F (the frizzled/smoothened receptor family). Nearly 800 human GPCR genes have been identified and are involved essentially in all major physiological processes. Approximately 40% of clinically marketed drugs mediate their effects through modulation of GPCR function for the treatment of a variety of human diseases including bacterial infections. Pssm-ID: 410628 [Multi-domain] Cd Length: 267 Bit Score: 40.87 E-value: 6.37e-04
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| 7tmA_NPBWR | cd15087 | neuropeptide B/W receptors, member of the class A family of seven-transmembrane G ... |
75-325 | 6.47e-04 | |||||
neuropeptide B/W receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Neuropeptide B/W receptor 1 and 2 are members of the class A G-protein coupled receptors that bind the neuropeptides B and W, respectively. NPBWR1 (previously known as GPR7) is expressed predominantly in cerebellum and frontal cortex, while NPBWR2 (previously known as GPR8) is located mostly in the frontal cortex and is present in human, but not in rat and mice. These receptors are suggested to be involved in the regulation of food intake, neuroendocrine function, and modulation of inflammatory pain, among many others. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320215 [Multi-domain] Cd Length: 282 Bit Score: 40.88 E-value: 6.47e-04
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| 7tmA_5-HT2C | cd15305 | serotonin receptor subtype 2C, member of the class A family of seven-transmembrane G ... |
79-327 | 1.02e-03 | |||||
serotonin receptor subtype 2C, member of the class A family of seven-transmembrane G protein-coupled receptors; The 5-HT2 receptors are a subfamily of serotonin receptors that bind the neurotransmitter serotonin (5HT; 5-hydroxytryptamine) in the central nervous system (CNS). The 5-HT2 subfamily is composed of three subtypes that mediate excitatory neurotransmission: 5-HT2A, 5-HT2B, and 5-HT2C. They are selectively linked to G proteins of the G(q/11) family and activate phospholipase C, which leads to activation of protein kinase C and calcium release. In the CNS, serotonin is involved in the regulation of appetite, mood, sleep, cognition, learning and memory, as well as implicated in diseases such as migraine, schizophrenia, and depression. Indeed, 5-HT2 receptors are attractive targets for a variety of psychoactive drugs, ranging from atypical antipsychotic drugs, antidepressants, and anxiolytics, which have an antagonistic action on 5-HT2 receptors, to hallucinogens, which act as agonists at postsynaptic 5-HT2 receptors. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 341346 [Multi-domain] Cd Length: 275 Bit Score: 40.27 E-value: 1.02e-03
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| 7tmA_GPR171 | cd15167 | orphan G protein-coupled receptor 171, member of the class A family of seven-transmembrane G ... |
114-327 | 1.23e-03 | |||||
orphan G protein-coupled receptor 171, member of the class A family of seven-transmembrane G protein-coupled receptors; GPR171 is phylogenetically related to the P2Y family of purinergic G protein-coupled receptors. The P2Y receptor family is composed of eight subtypes, which are activated by naturally occurring extracellular nucleotides such as ATP, ADP, UTP, UDP, and UDP-glucose. A recent study has been reported that the peptide LENSSPQAPARRLLPP (BigLEN) activates GPR17 to regulate body weight in mice; however the biological role of the receptor remains unknown. GPR171 is a member of the class A G protein-coupled receptor superfamily, which all have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A common feature of GPCR signaling is agonist-induced conformational changes in the receptors, which then activate the heterotrimeric G proteins. G-proteins regulate a variety of cellular functions including metabolic enzymes, ion channels, and transporters, among many others. Pssm-ID: 320295 [Multi-domain] Cd Length: 282 Bit Score: 40.13 E-value: 1.23e-03
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| 7tmA_alpha-2D_AR | cd15324 | alpha-2 adrenergic receptors subtype D, member of the class A family of seven-transmembrane G ... |
78-327 | 1.33e-03 | |||||
alpha-2 adrenergic receptors subtype D, member of the class A family of seven-transmembrane G protein-coupled receptors; The alpha-2 adrenergic receptors (or adrenoceptors) are a subfamily of the class A rhodopsin-like GPCRs that share a common architecture of seven transmembrane helices. This subfamily consists of three highly homologous receptor subtypes that have a key role in neurotransmitter release: alpha-2A, alpha-2B, and alpha-2C. In addition, a fourth subtype, alpha-2D is present in ray-finned fishes and amphibians, but is not found in humans. The alpha-2 receptors are found in both central and peripheral nervous system and serve to produce inhibitory functions through the G(i) proteins. Thus, the alpha-2 receptors inhibit adenylate cyclase, which decreases cAMP production and thereby decreases calcium influx during the action potential. Consequently, lowered levels of calcium will lead to a decrease in neurotransmitter release by negative feedback. Pssm-ID: 320447 [Multi-domain] Cd Length: 256 Bit Score: 39.85 E-value: 1.33e-03
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| 7tmA_P2Y13 | cd15151 | P2Y purinoceptor 13, member of the class A family of seven-transmembrane G protein-coupled ... |
107-323 | 1.50e-03 | |||||
P2Y purinoceptor 13, member of the class A family of seven-transmembrane G protein-coupled receptors; The P2Y13 receptor (P2Y13R) is activated by adenosine diphosphate (ADP) and belongs to the G(i) class of the P2Y family of purinergic G protein-coupled receptors. P2Y receptor family is composed of eight subtypes, which are activated by naturally occurring extracellular nucleotides such as ATP, ADP, UTP, UDP, and UDP-sugars. These eight receptors are ubiquitous in human tissues and can be further classified into two subfamilies based on sequence homology and second messenger coupling: a subfamily of five P2Y1-like receptors (P2Y1, P2Y2, P2Y4, P2Y6, and P2Y11Rs) that are coupled to G(q) protein to activate phospholipase C (PLC) and a second subfamily of three P2Y12-like receptors (P2Y12, P2YR13, and P2Y14Rs) that are coupled to G(i) protein to inhibit adenylate cyclase. Several cloned subtypes, such as P2Y3, P2Y5 and P2Y7-10, are not functional mammalian nucleotide receptors. The native agonists for P2Y receptors are: ATP (P2Y2, P2Y12), ADP (P2Y1, P2Y12 and P2Y13), UTP (P2Y2, P2Y4), UDP (P2Y6, P2Y14), and UDP-sugars (P2Y14). Pssm-ID: 341327 Cd Length: 284 Bit Score: 39.76 E-value: 1.50e-03
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| 7tmA_VA_opsin | cd15082 | non-visual VA (vertebrate ancient) opsins, member of the class A family of seven-transmembrane ... |
79-288 | 1.70e-03 | |||||
non-visual VA (vertebrate ancient) opsins, member of the class A family of seven-transmembrane G protein-coupled receptors; The vertebrate ancient (VA) opsin photopigments were originally identified in salmon and they appear to have diverged early in the evolution of vertebrate opsins. VA opsins are localized in the inner retina and the brain in teleosts. The vertebrate non-visual opsin family includes pinopsins, parapinopsin, VA (vertebrate ancient) opsins, and parietopsins. These non-visual opsins are expressed in various extraretinal tissues and/or in non-rod, non-cone retinal cells. They are thought to be involved in light-dependent physiological functions such as photo-entrainment of circadian rhythm, photoperiodicity, and body color change. The VA opsins belong the class A of the G protein-coupled receptors and possess seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. Pssm-ID: 320210 [Multi-domain] Cd Length: 291 Bit Score: 39.39 E-value: 1.70e-03
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| 7tmA_ET_R | cd15128 | endothelin receptors, member of the class A family of seven-transmembrane G protein-coupled ... |
79-327 | 1.82e-03 | |||||
endothelin receptors, member of the class A family of seven-transmembrane G protein-coupled receptors; Endothelins are 21-amino acid peptides which able to activate a number of signal transduction processes including phospholipase A2, phospholipase C, and phospholipase D, as well as cytosolic protein kinase activation. They play an important role in the regulation of the cardiovascular system and are the most potent vasoconstrictors identified, stimulating cardiac contraction, regulating the release of vasoactive substances, and stimulating mitogenesis in blood vessels. Two endothelin receptor subtypes have been isolated and identified in vertebrates, endothelin A receptor (ET-A) and endothelin B receptor (ET-B), and are members of the seven transmembrane class A G-protein coupled receptor family which activate multiple effectors via different types of G protein. Some vertebrates contain a third subtype, endothelin A receptor (ET-C). ET-A receptors are mainly located on vascular smooth muscle cells, whereas ET-B receptors are present on endothelial cells lining the vessel wall. Endothelin receptors have also been found in the brain. Pssm-ID: 320256 [Multi-domain] Cd Length: 300 Bit Score: 39.43 E-value: 1.82e-03
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| 7tm_classB | cd13952 | class B family of seven-transmembrane G protein-coupled receptors; The class B of ... |
103-315 | 2.17e-03 | |||||
class B family of seven-transmembrane G protein-coupled receptors; The class B of seven-transmembrane GPCRs is classified into three major subfamilies: subfamily B1 (secretin-like receptor family), B2 (adhesion family), and B3 (Methuselah-like family). The class B receptors have been identified in all the vertebrates, from fishes to mammals, as well as invertebrates including Caenorhabditis elegans and Drosophila melanogaster, but are not present in plants, fungi or prokaryotes. The B1 subfamily comprises receptors for polypeptide hormones of 27-141 amino-acid residues such as secretin, glucagon, glucagon-like peptide (GLP), calcitonin gene-related peptide, parathyroid hormone (PTH), and corticotropin-releasing factor. These receptors contain the large N-terminal extracellular domain (ECD), which plays a critical role in hormone recognition by binding to the C-terminal portion of the peptide. On the other hand, the N-terminal segment of the hormone induces receptor activation by interacting with the receptor transmembrane domains and connecting extracellular loops, triggering intracellular signaling pathways. All members of the subfamily B1 receptors preferentially couple to G proteins of G(s) family, which positively stimulate adenylate cyclase, leading to increased intracellular cAMP formation and calcium influx. The subfamily B2 consists of cell-adhesion receptors with 33 members in humans and vertebrates. The adhesion receptors are characterized by the presence of large N-terminal extracellular domains containing a variety of structural motifs, which play critical roles in cell-cell adhesion and cell-matrix interactions, linked to a class B seven-transmembrane domain. These include, for example, EGF (epidermal growth factor)-like domains in CD97, Celsr1 (cadherin family member), Celsr2, Celsr3, EMR1 (EGF-module-containing mucin-like hormone receptor-like 1), EMR2, EMR3, and Flamingo; two laminin A G-type repeats and nine cadherin domains in Flamingo and its human orthologs Celsr1, Celsr2 and Celsr3; olfactomedin-like domains in the latrotoxin receptors; and five or four thrombospondin type 1 repeats in BAI1 (brain-specific angiogenesis inhibitor 1), BAI2 and BAI3. Almost all adhesion receptors, except GPR123, contain an evolutionarily conserved GPCR- autoproteolysis inducing (GAIN) domain that undergoes autoproteolytic processing at the GPCR proteolysis site (GPS) motif located immediately N-terminal to the first transmembrane region, to generate N- and C-terminal fragments (NTF and CTF), which may serve important biological functions. Furthermore, the subfamily B3 includes Methuselah (Mth) protein, which was originally identified in Drosophila as a GPCR affecting stress resistance and aging, and its closely related proteins. Pssm-ID: 410627 [Multi-domain] Cd Length: 260 Bit Score: 39.12 E-value: 2.17e-03
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| 7tmA_FP | cd15145 | prostaglandin F2-alpha receptor, member of the class A family of seven-transmembrane G ... |
112-285 | 2.28e-03 | |||||
prostaglandin F2-alpha receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; The PGF2-alpha receptor, also called prostanoid FP receptor, is a class A G-protein coupled receptor whose endogenous ligand is prostaglandin F2-alpha. PGF2-alpha binding to this receptor is coupled to the stimulation of phospholipase C (PLC) pathway via G-protein subunit G(q). This leads to the release of inositol trisphosphate (IP3) and diacylglycerol (DAG) which results in increased intracellular Ca2+ levels and activation of PKC. The receptor activation primarily induces uterine contraction and bronchoconstriction, and stimulates luteolysis. Like most prostanoid receptors, the PGF2-alpha receptor has also been implicated in tumor angiogenesis and metastasis. Pssm-ID: 320273 [Multi-domain] Cd Length: 290 Bit Score: 39.04 E-value: 2.28e-03
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| 7tmA_ET-CR | cd15977 | endothelin C receptor, member of the class A family of seven-transmembrane G protein-coupled ... |
78-288 | 2.94e-03 | |||||
endothelin C receptor, member of the class A family of seven-transmembrane G protein-coupled receptors; Endothelins are able to activate a number of signal transduction processes including phospholipase A2, phospholipase C, and phospholipase D, as well as cytosolic protein kinase activation. They play an important role in the regulation of the cardiovascular system and are the most potent vasoconstrictors identified, stimulating cardiac contraction, regulating the release of vasoactive substances, and stimulating mitogenesis in blood vessels. Two endothelin receptor subtypes have been isolated and identified in vertebrates, endothelin A receptor (ET-A) and endothelin B receptor (ET-B), and are members of the seven transmembrane class A G-protein coupled receptor family which activate multiple effectors via different types of G protein. Some vertebrates contain a third subtype, endothelin A receptor (ET-C). ET-A receptors are mainly located on vascular smooth muscle cells, whereas ET-B receptors are present on endothelial cells lining the vessel wall. Endothelin receptors have also been found in the brain. The ET-C receptor is specific for endothelin-3 on frog dermal melanophores; its activation causes dispersion of pigment granules. Pssm-ID: 320643 [Multi-domain] Cd Length: 296 Bit Score: 38.73 E-value: 2.94e-03
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| 7tmA_P2Y8 | cd15368 | purinergic receptor P2Y8, member of the class A family of seven-transmembrane G ... |
107-327 | 3.02e-03 | |||||
purinergic receptor P2Y8, member of the class A family of seven-transmembrane G protein-coupled receptors; P2Y8 (or P2RY8) expression is often increased in leukemia patients, and it plays a role in the pathogenesis of acute leukemia. P2Y8 is phylogenetically closely related to the protease-activated receptors (PARs), which are activated by serine proteases such as thrombin, trypsin, and tryptase. These proteases cleave the extracellular domain of the receptor to form a new N-terminus, which in turn functions as a tethered ligand. The newly-formed tethered ligand binds intramolecularly to activate the receptor and triggers G-protein binding and intracellular signaling. Four different types of the protease-activated receptors have been identified (PAR1-4) and are predominantly expressed in platelets. PAR1, PA3, and PAR4 are activated by thrombin, whereas PAR2 is activated by trypsin. The PARs are known to couple with several G-proteins including Gi (cAMP inhibitory), G12/13 (Rho and Ras activation), and Gq (calcium signaling) to activate downstream signaling messengers which induces numerous cellular and physiological effects. Pssm-ID: 320490 [Multi-domain] Cd Length: 281 Bit Score: 38.60 E-value: 3.02e-03
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| 7tmA_SREB-like | cd15005 | super conserved receptor expressed in brain and related proteins, member of the class A family ... |
79-173 | 3.31e-03 | |||||
super conserved receptor expressed in brain and related proteins, member of the class A family of seven-transmembrane G protein-coupled receptors; The SREB (super conserved receptor expressed in brain) subfamily consists of at least three members, named SREB1 (GPR27), SREB2 (GPR85), and SREB3 (GPR173). They are very highly conserved G protein-coupled receptors throughout vertebrate evolution, however no endogenous ligands have yet been identified. SREB2 is greatly expressed in brain regions involved in psychiatric disorders and cognition, such as the hippocampal dentate gyrus. Genetic studies in both humans and mice have shown that SREB2 influences brain size and negatively regulates hippocampal adult neurogenesis and neurogenesis-dependent cognitive function, all of which are suggesting a potential link between SREB2 and schizophrenia. All three SREB genes are highly expressed in differentiated hippocampal neural stem cells. Furthermore, all GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320134 [Multi-domain] Cd Length: 329 Bit Score: 38.98 E-value: 3.31e-03
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| 7tmA_CCR9 | cd15174 | CC chemokine receptor type 9, member of the class A family of seven-transmembrane G ... |
71-283 | 3.36e-03 | |||||
CC chemokine receptor type 9, member of the class A family of seven-transmembrane G protein-coupled receptors; CCR9 is a homeostatic receptor specific for CCL25 (formerly known as thymus expressed chemokine) and is highly expressed on both immature and mature thymocytes as well as on intestinal homing T Lymphocytes and mucosal Lymphocytes. In cutaneous melanoma, activation of CCR9-CCL25 has been shown to stimulate metastasis to the small intestine. Chemokines are principal regulators for leukocyte trafficking, recruitment, and activation. Chemokine family membership is defined on the basis of sequence homology and on the presence of variations on a conserved cysteine motif, which allows the family to further divide into four subfamilies (CC, CXC, XC, and CX3C). Chemokines interact with seven-transmembrane receptors which are typically coupled to G protein for signaling. Currently, there are ten known receptors for CC chemokines, seven for CXC chemokines, and single receptors for the XC and CX3C chemokines. The CC chemokine receptors are all activating the G protein Gi. Pssm-ID: 320302 [Multi-domain] Cd Length: 280 Bit Score: 38.58 E-value: 3.36e-03
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| 7tmA_CX3CR1 | cd15186 | CX3C chemokine receptor 1, member of the class A family of seven-transmembrane G ... |
70-325 | 3.69e-03 | |||||
CX3C chemokine receptor 1, member of the class A family of seven-transmembrane G protein-coupled receptors; CX3CR1 is an inflammatory receptor specific for CX3CL1 (also known as fractalkine in human), which is involved in the adhesion and migration of leukocytes. The CX3C chemokine subfamily is only represented by CX3CL1, which exists in both soluble and membrane-anchored forms. Membrane-anchored form promotes strong adhesion of receptor-bearing leukocytes to CX3CL1-expressing endothelial cells. On the other hand, soluble CX3CL1, which is released by the proteolytic cleavage of membrane-anchored CX3CL1, is a potent chemoattractant for CX3CR1-expressing T cells and monocytes. Chemokine family membership is defined on the basis of sequence homology and on the presence of variations on a conserved cysteine motif, which allows the family to further divide into four subfamilies (CC, CXC, XC, and CX3C). Chemokines interact with seven-transmembrane receptors which are typically coupled to G protein for signaling. Pssm-ID: 320314 [Multi-domain] Cd Length: 273 Bit Score: 38.28 E-value: 3.69e-03
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| 7tmA_GPR161 | cd15214 | orphan G protein-coupled receptor 161, member of the class A family of seven-transmembrane G ... |
83-324 | 6.70e-03 | |||||
orphan G protein-coupled receptor 161, member of the class A family of seven-transmembrane G protein-coupled receptors; GPR161, an orphan GPCR, is a negative regulator of Sonic hedgehog (Shh) signaling, which promotes the processing of zinc finger protein GLI3 into its transcriptional repressor form (GLI3R) during neural tube development. In the absence of Shh, this proteolytic processing is normally mediated by cAMP-dependent protein kinase A (PKA). GPR161 is recruited to primary cilia by a mechanism depends on TULP3 (tubby-related protein 3) and the intraflagellar complex A (IFT-A). Moreover, Gpr161 knockout mice show phenotypes observed in Tulp3/IFT-A mutants, and cause increased Shh signaling in the neural tube. Taken together, GPR161 negatively regulates the PKA-dependent GLI3 processing in the absence of Shh signal by coupling to G(s) protein, which causes activation of adenylate cyclase, elevated cAMP levels, and activation of PKA. Conversely, in the presence of Shh, GPR161 is removed from the cilia by internalization into the endosomal recycling compartment, leading to downregulation of its activity and thereby allowing Shh signaling to proceed. In addition, GPR161 is over-expressed in triple-negative breast cancer (lacking estrogen receptor, progesterone receptor, and human epidermal growth factor receptor 2 (HER2) expression) and correlates with poor prognosis. Mutations of GPR161 have also been implicated as a novel cause for pituitary stalk interruption syndrome (PSIS), a rare congenital disease of the pituitary gland. GPR161 is a member of the class A family of GPCRs, which contains receptors for hormones, neurotransmitters, sensory stimuli, and a variety of other ligands. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 320342 [Multi-domain] Cd Length: 261 Bit Score: 37.61 E-value: 6.70e-03
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| 7tmA_D4_dopamine_R | cd15308 | D4 dopamine receptor of the D2-like family, member of the class A family of ... |
83-288 | 8.76e-03 | |||||
D4 dopamine receptor of the D2-like family, member of the class A family of seven-transmembrane G protein-coupled receptors; Dopamine receptors are members of the class A G protein-coupled receptors that are involved in many neurological processes in the central nervous system (CNS). The neurotransmitter dopamine is the primary endogenous agonist for dopamine receptors. Dopamine receptors consist of at least five subtypes: D1, D2, D3, D4, and D5. The D1 and D5 subtypes are members of the D1-like family of dopamine receptors, whereas the D2, D3 and D4 subtypes are members of the D2-like family. Activation of D2-like family receptors is linked to G proteins of the G(i) family. This leads to a decrease in adenylate cyclase activity, thereby decreasing cAMP levels. Dopamine receptors are major therapeutic targets for neurological and psychiatric disorders such as drug abuse, depression, schizophrenia, or Parkinson's disease. Pssm-ID: 320434 [Multi-domain] Cd Length: 258 Bit Score: 37.12 E-value: 8.76e-03
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| 7tmA_5-HT2A | cd15304 | serotonin receptor subtype 2A, member of the class A family of seven-transmembrane G ... |
79-327 | 9.40e-03 | |||||
serotonin receptor subtype 2A, member of the class A family of seven-transmembrane G protein-coupled receptors; The 5-HT2 receptors are a subfamily of serotonin receptors that bind the neurotransmitter serotonin (5HT; 5-hydroxytryptamine) in the central nervous system (CNS). The 5-HT2 subfamily is composed of three subtypes that mediate excitatory neurotransmission: 5-HT2A, 5-HT2B, and 5-HT2C. They are selectively linked to G proteins of the G(q/11) family and activate phospholipase C, which leads to activation of protein kinase C and calcium release. In the CNS, serotonin is involved in the regulation of appetite, mood, sleep, cognition, learning and memory, as well as implicated in diseases such as migraine, schizophrenia, and depression. Indeed, 5-HT2 receptors are attractive targets for a variety of psychoactive drugs, ranging from atypical antipsychotic drugs, antidepressants, and anxiolytics, which have an antagonistic action on 5-HT2 receptors, to hallucinogens, which act as agonists at postsynaptic 5-HT2 receptors. All GPCRs have a common structural architecture comprising of seven-transmembrane (TM) alpha-helices interconnected by three extracellular and three intracellular loops. A general feature of GPCR signaling is agonist-induced conformational changes in the receptors, leading to activation of the heterotrimeric G proteins, which consist of the guanine nucleotide-binding G-alpha subunit and the dimeric G-beta-gamma subunits. The activated G proteins then bind to and activate numerous downstream effector proteins, which generate second messengers that mediate a broad range of cellular and physiological processes. Pssm-ID: 341345 [Multi-domain] Cd Length: 267 Bit Score: 37.22 E-value: 9.40e-03
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