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    GRK3 G protein-coupled receptor kinase 3 [ Homo sapiens (human) ]

    Gene ID: 157, updated on 10-Oct-2024

    GeneRIFs: Gene References Into Functions

    GeneRIFPubMed TitleDate
    A novel GRK3-HDAC2 regulatory pathway is a key direct link between neuroendocrine differentiation and angiogenesis in prostate cancer progression.

    A novel GRK3-HDAC2 regulatory pathway is a key direct link between neuroendocrine differentiation and angiogenesis in prostate cancer progression.
    Naderinezhad S, Zhang G, Wang Z, Zheng D, Hulsurkar M, Bakhoum M, Su N, Yang H, Shen T, Li W., Free PMC Article

    09/1/2023
    Aged G Protein-Coupled Receptor Kinase 3 (Grk3)-Deficient Mice Exhibit Enhanced Osteoclastogenesis and Develop Bone Lesions Analogous to Human Paget's Disease of Bone.

    Aged G Protein-Coupled Receptor Kinase 3 (Grk3)-Deficient Mice Exhibit Enhanced Osteoclastogenesis and Develop Bone Lesions Analogous to Human Paget's Disease of Bone.
    Rabjohns EM, Rampersad RR, Ghosh A, Hurst K, Eudy AM, Brozowski JM, Lee HH, Ren Y, Mirando A, Gladman J, Bowser JL, Berg K, Wani S, Ralston SH, Hilton MJ, Tarrant TK., Free PMC Article

    04/19/2023
    TEAD3 inhibits the proliferation and metastasis of prostate cancer via suppressing ADRBK2.

    TEAD3 inhibits the proliferation and metastasis of prostate cancer via suppressing ADRBK2.
    Wang C, Chen S, Li X, Fan L, Zhou Z, Zhang M, Shao Y, Shang Z, Niu Y.

    03/28/2023
    Dissecting the roles of GRK2 and GRK3 in mu-opioid receptor internalization and beta-arrestin2 recruitment using CRISPR/Cas9-edited HEK293 cells.

    Dissecting the roles of GRK2 and GRK3 in μ-opioid receptor internalization and β-arrestin2 recruitment using CRISPR/Cas9-edited HEK293 cells.
    Møller TC, Pedersen MF, van Senten JR, Seiersen SD, Mathiesen JM, Bouvier M, Bräuner-Osborne H., Free PMC Article

    03/13/2021
    RKIP has several binding sites within the N-termini of GRK3.The N-termini of GRK3 binds to beta2-adrenoceptors.

    The N-termini of GRK2 and GRK3 simulate the stimulating effects of RKIP on β-adrenoceptors.
    Maimari T, Krasel C, Bünemann M, Lorenz K.

    07/25/2020
    Study found that GRK3 was significantly overexpressed in 162 pairs of colon cancer tissues than in the matched noncancerous mucosa. These data show that aberrant expression of GRK3 plays an important role in promoting colon cancer progression through enhanced proliferation and reduced apoptosis.

    Overexpression of GRK3, Promoting Tumor Proliferation, Is Predictive of Poor Prognosis in Colon Cancer.
    Jiang T, Yang C, Ma L, Wu Z, Ye L, Ma X, Li H, Fan J, Yang Y., Free PMC Article

    09/15/2018
    hat expression of GRK3 was down-regulated in pancreatic ductal adenocarcinoma and was an independent prognostic factor

    High expression of GRK3 is associated with favorable prognosis in pancreatic ductal adenocarcinoma.
    Liu WJ, Zhou L, Liang ZY, Zhou WX, You L, Zhang TP, Zhao YP.

    09/1/2018
    GRK3 is a new critical activator of neuroendocrine phenotypes and mediator of CREB activation in promoting neuroendocrine differentiation of prostate cancer cells.

    GRK3 is a direct target of CREB activation and regulates neuroendocrine differentiation of prostate cancer cells.
    Sang M, Hulsurkar M, Zhang X, Song H, Zheng D, Zhang Y, Li M, Xu J, Zhang S, Ittmann M, Li W., Free PMC Article

    02/10/2018
    effects of GRK3 modulation appear to be specific to chemokine-mediated migration behaviors without influencing tumor cell proliferation or survival

    G Protein Coupled Receptor Kinase 3 Regulates Breast Cancer Migration, Invasion, and Metastasis.
    Billard MJ, Fitzhugh DJ, Parker JS, Brozowski JM, McGinnis MW, Timoshchenko RG, Serafin DS, Lininger R, Klauber-Demore N, Sahagian G, Truong YK, Sassano MF, Serody JS, Tarrant TK., Free PMC Article

    08/27/2016
    data are consistent with the possibility that oncogenes can induce cellular stiffness via an HDAC6-induced reorganization of the vimentin intermediate filament network

    GRK3 is essential for metastatic cells and promotes prostate tumor progression.
    Li W, Ai N, Wang S, Bhattacharya N, Vrbanac V, Collins M, Signoretti S, Hu Y, Boyce FM, Gravdal K, Halvorsen OJ, Nalwoga H, Akslen LA, Harlow E, Watnick RS., Free PMC Article

    05/10/2014
    Data indicate that CXCL12-induced phosphorylation at CXCR4 S346/347 was mediated by GRK2/3.

    Hierarchical organization of multi-site phosphorylation at the CXCR4 C terminus.
    Mueller W, Schütz D, Nagel F, Schulz S, Stumm R., Free PMC Article

    01/11/2014
    In oral squamous cell carcinomas, malignant cells and surrounding tissue overexpress the ADRBK2 gene.

    Activity of β2-adrenergic receptor in oral squamous cell carcinoma is mediated by overexpression of the ADRBK2 gene: a pilot study.
    Pérez-Sayáns M, Somoza-Martín JM, Barros-Angueira F, Gayoso-Diz P, Otero-Rey EM, Gándra-Rey JM, García-García A.

    07/21/2012
    A reduced cortical concentration of GRK3 in schizophrenia (resembling that in aging) may result in altered G protein-dependent signaling, thus contributing to prefrontal deficits in schizophrenia.

    Reduced expression of G protein-coupled receptor kinases in schizophrenia but not in schizoaffective disorder.
    Bychkov ER, Ahmed MR, Gurevich VV, Benovic JL, Gurevich EV., Free PMC Article

    06/16/2012
    GRK3 is a negative regulator of cell growth whose expression is preferentially reduced in glioblastoma of the classical subtype as a consequence of activity in primary gliomagenic pathways.

    Suppression of G-protein-coupled receptor kinase 3 expression is a feature of classical GBM that is required for maximal growth.
    Woerner BM, Luo J, Brown KR, Jackson E, Dahiya SM, Mischel P, Benovic JL, Piwnica-Worms D, Rubin JB., Free PMC Article

    05/26/2012
    Observational study of gene-disease association, gene-environment interaction, and pharmacogenomic / toxicogenomic. (HuGE Navigator)

    Variation at the NFATC2 locus increases the risk of thiazolidinedione-induced edema in the Diabetes REduction Assessment with ramipril and rosiglitazone Medication (DREAM) study.
    Bailey SD, Xie C, Do R, Montpetit A, Diaz R, Mohan V, Keavney B, Yusuf S, Gerstein HC, Engert JC, Anand S, DREAM investigators., Free PMC Article

    09/15/2010
    mRNA levels for GRK3 were inversely correlated with systolic and diastolic blood pressure (day, night and 24 h), which suggests a protective role for GRK3 in the regulation of human blood pressure

    beta-Adrenoceptor and GRK3 expression in human lymphocytes is related to blood pressure and urinary albumin excretion.
    Oliver E, Rovira E, Montó F, Valldecabres C, Julve R, Muedra V, Ruiz N, Barettino D, D'Ocon P.

    08/23/2010
    Clinical trial of gene-disease association and gene-environment interaction. (HuGE Navigator)

    Personalized smoking cessation: interactions between nicotine dose, dependence and quit-success genotype score.
    Rose JE, Behm FM, Drgon T, Johnson C, Uhl GR., Free PMC Article

    06/30/2010
    we found no evidence of altered levels of acetylated histone H3 at the affected allele compared to the common allele

    Allele specific analysis of the ADRBK2 gene in lymphoblastoid cells from bipolar disorder patients.
    McCarthy MJ, Barrett TB, Nissen S, Kelsoe JR, Turner EE., Free PMC Article

    05/31/2010
    The G-384A variant may alter binding of Sp1/Sp4 transcription factors resulting in an increase in gene transcription and an increase in vulnerability to bipolar disorder.

    Promoter variant in the GRK3 gene associated with bipolar disorder alters gene expression.
    Zhou X, Barrett TB, Kelsoe JR., Free PMC Article

    01/21/2010
    role for GRK3 in regulating CXCR4 attenuation and have provided a mechanistic link between the GRK3 pathway and the CXCR4-related WHIM(WT) disorder.

    Leukocyte analysis from WHIM syndrome patients reveals a pivotal role for GRK3 in CXCR4 signaling.
    Balabanian K, Levoye A, Klemm L, Lagane B, Hermine O, Harriague J, Baleux F, Arenzana-Seisdedos F, Bachelerie F., Free PMC Article

    01/21/2010
    Observational study of gene-disease association. (HuGE Navigator)See all PubMed (8) articles

    A large-scale candidate gene association study of age at menarche and age at natural menopause.
    He C, Kraft P, Chasman DI, Buring JE, Chen C, Hankinson SE, Paré G, Chanock S, Ridker PM, Hunter DJ.

    Association study of 182 candidate genes in anorexia nervosa.
    Pinheiro AP, Bulik CM, Thornton LM, Sullivan PF, Root TL, Bloss CS, Berrettini WH, Schork NJ, Kaye WH, Bergen AW, Magistretti P, Brandt H, Crawford S, Crow S, Fichter MM, Goldman D, Halmi KA, Johnson C, Kaplan AS, Keel PK, Klump KL, La Via M, Mitchell JE, Strober M, Rotondo A, Treasure J, Woodside DB.

    Comprehensive copy number variant (CNV) analysis of neuronal pathways genes in psychiatric disorders identifies rare variants within patients.
    Saus E, Brunet A, Armengol L, Alonso P, Crespo JM, Fernández-Aranda F, Guitart M, Martín-Santos R, Menchón JM, Navinés R, Soria V, Torrens M, Urretavizcaya M, Vallès V, Gratacòs M, Estivill X.

    Gene-centric association signals for lipids and apolipoproteins identified via the HumanCVD BeadChip.
    Talmud PJ, Drenos F, Shah S, Shah T, Palmen J, Verzilli C, Gaunt TR, Pallas J, Lovering R, Li K, Casas JP, Sofat R, Kumari M, Rodriguez S, Johnson T, Newhouse SJ, Dominiczak A, Samani NJ, Caulfield M, Sever P, Stanton A, Shields DC, Padmanabhan S, Melander O, Hastie C, Delles C, Ebrahim S, Marmot MG, Smith GD, Lawlor DA, Munroe PB, Day IN, Kivimaki M, Whittaker J, Humphries SE, Hingorani AD, ASCOT investigators, NORDIL investigators, BRIGHT Consortium.

    Identification of new putative susceptibility genes for several psychiatric disorders by association analysis of regulatory and non-synonymous SNPs of 306 genes involved in neurotransmission and neurodevelopment.
    Gratacòs M, Costas J, de Cid R, Bayés M, González JR, Baca-García E, de Diego Y, Fernández-Aranda F, Fernández-Piqueras J, Guitart M, Martín-Santos R, Martorell L, Menchón JM, Roca M, Sáiz-Ruiz J, Sanjuán J, Torrens M, Urretavizcaya M, Valero J, Vilella E, Estivill X, Carracedo A, Psychiatric Genetics Network Group.

    Further evidence for association of GRK3 to bipolar disorder suggests a second disease mutation.
    Barrett TB, Emberton JE, Nievergelt CM, Liang SG, Hauger RL, Eskin E, Schork NJ, Kelsoe JR, Barrett TB, Emberton JE, Nievergelt CM, Liang SG, Hauger RL, Eskin E, Schork NJ, Kelsoe JR.

    Association analysis of GRK3 gene promoter variants in cocaine abuse.
    Guindalini C, Collier D, Laranjeira R, Barrett TB, Kelsoe J, Castelo A, Vallada H, Breen G, Guindalini C, Collier D, Laranjeira R, Barrett TB, Kelsoe J, Castelo A, Vallada H, Breen G.

    Bipolar 1 disorder is not associated with the RGS4, PRODH, COMT and GRK3 genes.
    Prata DP, Breen G, Munro J, Sinclair M, Osborne S, Li T, Kerwin R, St Clair D, Collier DA.

    03/13/2008
    Dysregulation in GRK3 expression alters signaling desensitization and thereby predisposes to the development of bipolar disease.

    Further evidence for association of GRK3 to bipolar disorder suggests a second disease mutation.
    Barrett TB, Emberton JE, Nievergelt CM, Liang SG, Hauger RL, Eskin E, Schork NJ, Kelsoe JR, Barrett TB, Emberton JE, Nievergelt CM, Liang SG, Hauger RL, Eskin E, Schork NJ, Kelsoe JR.

    01/21/2010
    No support for a major role for GRK3 gene promoter variants in cocaine addiction.

    Association analysis of GRK3 gene promoter variants in cocaine abuse.
    Guindalini C, Collier D, Laranjeira R, Barrett TB, Kelsoe J, Castelo A, Vallada H, Breen G, Guindalini C, Collier D, Laranjeira R, Barrett TB, Kelsoe J, Castelo A, Vallada H, Breen G.

    01/21/2010
    ATP stimulation leads to GRK3 phosphorylation of P2X(7) receptor.

    ATP stimulates GRK-3 phosphorylation and beta-arrestin-2-dependent internalization of P2X7 receptor.
    Feng YH, Wang L, Wang Q, Li X, Zeng R, Gorodeski GI., Free PMC Article

    01/21/2010
    the CRH-R1alpha carboxyl tail is important for regulation of receptor activity by G protein-coupled receptor kinase

    Regulation of corticotropin-releasing hormone receptor type 1alpha signaling: structural determinants for G protein-coupled receptor kinase-mediated phosphorylation and agonist-mediated desensitization.
    Teli T, Markovic D, Levine MA, Hillhouse EW, Grammatopoulos DK.

    01/21/2010
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