4YAY,4ZUD


Conserved Protein Domain Family
7tmA_AT1R

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cd15192: 7tmA_AT1R 
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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.
Statistics
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PSSM-Id: 320320
Aligned: 9 rows
Threshold Bit Score: 445.723
Created: 11-Dec-2008
Updated: 25-Oct-2021
Structure
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Program:
Drawing:
Aligned Rows:
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Conserved site includes 17 residues -Click on image for an interactive view with Cn3D
Feature 1:putative peptide ligand binding pocket [polypeptide binding site]
Evidence:
  • Comment:based on the structures of some angiotensin receptor family (class A) members with bound ligands (agonist peptides or chemical compound agonists/antagonists)
  • Comment:Small-molecule chemical ligands tend to bind deeper within the receptor core, compared to a peptide ligands, which binds towards the extracellular surface of its receptor.
  • Structure:4YAY: Human Type 1 Angiotensin Receptor binds selective antagonist ZD7155; contacts at 4A
  • Structure:4ZUD: Human angiotensin II type1 receptor (AT1R) binds an inverse agonist (Olmesartan), an highly potent anti-hypertensive drug; contacts at 4A

Sequence Alignment
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Format: Row Display: Color Bits: Type Selection:
Feature 1              #                                         #      #  ##   #            #  #
4YAY_A       124 VMIPTLYSIIFVVGIFGNSLVVIVIYFYMKLKtvASVFLLNLALADLCFLLTLPLWAVYTameYRWPFGnyLCKIASASV 203
4ZUD_A       124 VMIPTLYSIIFVVGIFGNSLVVIVIYFYMKLKtvASVFLLNLALADLCFLLTLPLWAVYTameYRWPFGnyLCKIASASV 203
CAF02299      32 LMIPVVYSIIFVIGVLGNSMVIIVIYYYLKLKtvANIFLLNLALADLTFVITLPLWAASTameYHWPFGvfLCKMSATVL 111 smaller spotted...
CAG04270      18 ILVPMVYGSIFVIGIVGNSMVVAVIYCYMKLKtvANIFVLNLAVSDLTFLITLPMWATSTakgYHWPFGefLCKASAGLV 97  Tetraodon nigro...
P79785        29 IMVPTVYSIIFIIGIFGNSLVVIVIYCYMKLKtvASIFLLNLALADLCFLITLPLWAAYTameYQWPFGncLCKLASAGI 108 chicken
P30556        29 VMIPTLYSIIFVVGIFGNSLVVIVIYFYMKLKtvASVFLLNLALADLCFLLTLPLWAVYTameYRWPFGnyLCKIASASV 108 human
XP_006007909  28 TMIPTIYGIIFVTGILGNSIVVAVIFCYMKLKtvANIFLFNLALADMIFLITLPLWAAYTamgYHWPFGncLCKISTALV 107 coelacanth
XP_007900643  23 LLIPITYSVIFVVGVIGNGLVVIVIYCYLKVItvANIFLLNLALADLIFIITLPVWAAYTamgYHWPFGgfLCKMCSTFV 102 elephant shark
P35373        31 ITIPIIYSTIFVVGVFGNSLVVIVIYSYMKMKtmASVFLMNLALSDLCFVITLPLWAVYTamhYHWPFGdlLCKIASTAI 110 African clawed ...
Feature 1        #  #                                                  #   #              #      
4YAY_A       204 SFNLYASVFLLTCLSIDRYLAIVHPmkSRLRRtmLVAKVTCIIIWLLAGLASLPAIIHRnvffientNITVCAFhyesq- 282
4ZUD_A       204 SFNLYASVFLLTCLSIDRYLAIVHPmkSRLRRtmLVAKVTCIIIWLLAGLASLPAIIHRnvffientNITVCAFhyesq- 282
CAF02299     112 LLNMNASIFLVTCLSVDRYLAIVHPikSRTKRtlVHAWMACIMVWILAGLASLPAMFFRdavhysdwNKTICAFhypkq- 190 smaller spotted...
CAG04270      98 IFNLYTSVFFLMALSIDRYLAIVHPvqSRRFRtvVYARVTCVVIWLFAFVLSLPTALTRdvhnisnvNMTVCGIlhnnie 177 Tetraodon nigro...
P79785       109 SFNLYASVFLLTCLSIDRYLAIVHPvkSRIRRtmFVARVTCIVIWLLAGVASLPVIIHRniffaenlNMTVCGFrydnn- 187 chicken
P30556       109 SFNLYASVFLLTCLSIDRYLAIVHPmkSRLRRtmLVAKVTCIIIWLLAGLASLPAIIHRnvffientNITVCAFhyesq- 187 human
XP_006007909 108 SYNLYATMFLLTCLSIDRYLAIVHPmkSRPRRtlIFARITCILAWLLAGVASIPVLIFRqviflknqNITVCSFfyke-- 185 coelacanth
XP_007900643 103 LINMNASIFLVTCLSIDRYLAIVHPmrSRSKRtlIQARVVCTVVWLLAAVTSLPNTFLRdtvsyeswNKTICAFqyper- 181 elephant shark
P35373       111 TLNLYTTVFLLTCLSIDRYSAIVHPmkSRIRRtvMVARLTCVGIWLVAFLASLPSVIYRqififpdtNQTVCALvyhsg- 189 African clawed ...
Feature 1                                                                           #  #         
4YAY_A       283 -nstlPIGLGLTKNILGFLFPFLIILTSYTLIWKALkkaye-iqknkPRNDDIFKIIMAIVLFFFFSWIPHQIFTFLDVL 360
4ZUD_A       283 -nstlPIGLGLTKNILGFLFPFLIILTSYTLIWKALkkaye-iqknkPRNDDIFKIIMAIVLFFFFSWIPHQIFTFLDVL 360
CAF02299     191 nrnqwVFGLALLKNLLGFLIPLLIILICYSLILKSLvqayq-ierskPVGNEAFKLIKAVVVSFILCWLPFQIFAFMDVL 269 smaller spotted...
CAG04270     178 slkelLLAISLMKSLLGFLIPFIVIITCYCLIGRALlsartiqkssrSRDDEVLRMLAAAVLAFFLCWAPHQVFHLMQFF 257 Tetraodon nigro...
P79785       188 -nttlRVGLGLSKNLLGFLIPFLIILTSYTLIWKTLkkayq-iqrnkTRNDDIFKMIVAIVFFFFFSWIPHQVFTFLDVL 265 chicken
P30556       188 -nstlPIGLGLTKNILGFLFPFLIILTSYTLIWKALkkaye-iqknkPRNDDIFKIIMAIVLFFFFSWIPHQIFTFLDVL 265 human
XP_006007909 186 -qdphLVVMGLMKNILGFFIPFAIILTCYTLIGKTLmetyk-vqknkSRCDEVLKVIMTVVVVFFICWFPHQVFNFLEVL 263 coelacanth
XP_007900643 182 hkeqwIFGMALLKILLGFLIPSFIILTCYFLILRSLmqayh-itrskQTNNEAFKVILAVVIMFLFCWLPYQIITFFDVL 260 elephant shark
P35373       190 -hiyfMVGMSLVKNIVGFFIPFVIILTSYTLIGKTLkevy---raqrARNDDIFKMIVAVVLLFFFCWIPHQVFTFLDVL 265 African clawed ...
Feature 1                              #   #                     
4YAY_A       361 IQlgiirdCRIADIVDTAMPITICIAYFNNCLNPLFYGFLGkkFKRYF 408
4ZUD_A       361 IQlgiirdCRIADIVDTAMPITICIAYFNNCLNPLFYGFLGkkFKRYF 408
CAF02299     270 SQlkiiksCHIPEVIDTSIPFTICVAYFNSCLNPILYGLVGrnFREKF 317 smaller spotted catshark
CAG04270     258 TQlkdadnCPLLEIIDTAMPFTICIAYFNSCVNPIVYGFVGhnFRKNL 305 Tetraodon nigroviridis
P79785       266 IQlhvitdCKITDIVDTAMPFTICIAYFNNCLNPFFYVFFGknFKKYF 313 chicken
P30556       266 IQlgiirdCRIADIVDTAMPITICIAYFNNCLNPLFYGFLGkkFKRYF 313 human
XP_006007909 264 VRlevitdCHIVNIVDTAMPFTICIAYFNSCLNPILYGFVGdnFRKKF 311 coelacanth
XP_007900643 261 FRlnviqnCYFSEMIDSSIPFTICLAYSNSCLNPILYGFVGhnFREKL 308 elephant shark
P35373       266 IQmdviqnCKMYDIVDTGMPITICIAYFNSCLNPFLYGFFGkkFRKHF 313 African clawed frog

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