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G protein-coupled receptor kinase 6

PDB rendering based on 2acx.
Available structures
Symbols GRK6; FLJ32135; GPRK6
External IDs OMIM600869 MGI1347078 HomoloGene37570 GeneCards: GRK6 Gene
RNA expression pattern
PBB GE GRK6 210981 s at tn.png
PBB GE GRK6 202848 s at tn.png
PBB GE GRK6 202849 x at tn.png
More reference expression data
Species Human Mouse
Entrez 2870 26385
Ensembl ENSG00000198055 ENSMUSG00000074886
UniProt P43250 Q9EPB9
RefSeq (mRNA) NM_001004105 NM_001038018
RefSeq (protein) NP_001004105 NP_001033107
Location (UCSC) Chr 5:
176.79 - 176.8 Mb
Chr 13:
55.46 - 55.47 Mb
PubMed search [1] [2]

G protein-coupled receptor kinase 6 is an enzyme that in humans is encoded by the GRK6 gene.[1][2]

This gene encodes a member of the guanine nucleotide-binding protein (G protein)-coupled receptor kinase subfamily of the Ser/Thr protein kinase family. The protein phosphorylates the activated forms of G protein-coupled receptors thus initiating their deactivation. Several transcript variants encoding different isoforms have been described for this gene.[2] GRK6 appears to be involved in responses to morphine.[3]


  1. ^ Haribabu B, Snyderman R (Nov 1993). "Identification of additional members of human G-protein-coupled receptor kinase multigene family". Proc Natl Acad Sci U S A 90 (20): 9398-402. PMID 8415712.  
  2. ^ a b "Entrez Gene: GRK6 G protein-coupled receptor kinase 6".  
  3. ^ Raehal KM, Schmid CL, Medvedev IO, Gainetdinov RR, Premont RT, Bohn LM (June 2009). "Morphine-induced physiological and behavioral responses in mice lacking G protein-coupled receptor kinase 6". Drug and Alcohol Dependence. doi:10.1016/j.drugalcdep.2009.04.011. PMID 19497686.  

Further reading

  • Bullrich F, Druck T, Kunapuli P, et al. (1995). "Chromosomal mapping of the genes GPRK5 and GPRK6 encoding G protein-coupled receptor kinases GRK5 and GRK6.". Cytogenet. Cell Genet. 70 (3-4): 250–4. doi:10.1159/000134045. PMID 7789183.  
  • Stoffel RH, Randall RR, Premont RT, et al. (1994). "Palmitoylation of G protein-coupled receptor kinase, GRK6. Lipid modification diversity in the GRK family.". J. Biol. Chem. 269 (45): 27791–4. PMID 7961702.  
  • Loudon RP, Benovic JL (1994). "Expression, purification, and characterization of the G protein-coupled receptor kinase GRK6.". J. Biol. Chem. 269 (36): 22691–7. PMID 8077221.  
  • Benovic JL, Gomez J (1993). "Molecular cloning and expression of GRK6. A new member of the G protein-coupled receptor kinase family.". J. Biol. Chem. 268 (26): 19521–7. PMID 8366096.  
  • Freedman NJ, Ament AS, Oppermann M, et al. (1997). "Phosphorylation and desensitization of human endothelin A and B receptors. Evidence for G protein-coupled receptor kinase specificity.". J. Biol. Chem. 272 (28): 17734–43. doi:10.1074/jbc.272.28.17734. PMID 9211925.  
  • Loudon RP, Benovic JL (1997). "Altered activity of palmitoylation-deficient and isoprenylated forms of the G protein-coupled receptor kinase GRK6.". J. Biol. Chem. 272 (43): 27422–7. doi:10.1074/jbc.272.43.27422. PMID 9341194.  
  • Stoffel RH, Inglese J, Macrae AD, et al. (1998). "Palmitoylation increases the kinase activity of the G protein-coupled receptor kinase, GRK6.". Biochemistry 37 (46): 16053–9. doi:10.1021/bi981432d. PMID 9819198.  
  • Premont RT, Claing A, Vitale N, et al. (1998). "beta2-Adrenergic receptor regulation by GIT1, a G protein-coupled receptor kinase-associated ADP ribosylation factor GTPase-activating protein.". Proc. Natl. Acad. Sci. U.S.A. 95 (24): 14082–7. doi:10.1073/pnas.95.24.14082. PMID 9826657.  
  • Milcent MD, Christophe T, Rabiet MJ, et al. (1999). "Overexpression of wild-type and catalytically inactive forms of GRK2 and GRK6 fails to alter the agonist-induced phosphorylation of the C5a receptor (CD88): evidence that GRK6 is autophosphorylated in COS-7 cells.". Biochem. Biophys. Res. Commun. 259 (1): 224–9. doi:10.1006/bbrc.1999.0758. PMID 10334944.  
  • Lazari MF, Liu X, Nakamura K, et al. (1999). "Role of G protein-coupled receptor kinases on the agonist-induced phosphorylation and internalization of the follitropin receptor.". Mol. Endocrinol. 13 (6): 866–78. doi:10.1210/me.13.6.866. PMID 10379886.  
  • Hall RA, Spurney RF, Premont RT, et al. (1999). "G protein-coupled receptor kinase 6A phosphorylates the Na(+)/H(+) exchanger regulatory factor via a PDZ domain-mediated interaction.". J. Biol. Chem. 274 (34): 24328–34. doi:10.1074/jbc.274.34.24328. PMID 10446210.  
  • Brenninkmeijer CB, Price SA, López Bernal A, Phaneuf S (1999). "Expression of G-protein-coupled receptor kinases in pregnant term and non-pregnant human myometrium.". J. Endocrinol. 162 (3): 401–8. doi:10.1677/joe.0.1620401. PMID 10467231.  
  • Premont RT, Macrae AD, Aparicio SA, et al. (1999). "The GRK4 subfamily of G protein-coupled receptor kinases. Alternative splicing, gene organization, and sequence conservation.". J. Biol. Chem. 274 (41): 29381–9. doi:10.1074/jbc.274.41.29381. PMID 10506199.  
  • Pronin AN, Morris AJ, Surguchov A, Benovic JL (2000). "Synucleins are a novel class of substrates for G protein-coupled receptor kinases.". J. Biol. Chem. 275 (34): 26515–22. doi:10.1074/jbc.M003542200. PMID 10852916.  
  • Tiruppathi C, Yan W, Sandoval R, et al. (2000). "G protein-coupled receptor kinase-5 regulates thrombin-activated signaling in endothelial cells.". Proc. Natl. Acad. Sci. U.S.A. 97 (13): 7440–5. doi:10.1073/pnas.97.13.7440. PMID 10861009.  
  • Zhou H, Yan F, Tai HH (2001). "Phosphorylation and desensitization of the human thromboxane receptor-alpha by G protein-coupled receptor kinases.". J. Pharmacol. Exp. Ther. 298 (3): 1243–51. PMID 11504827.  
  • Blaukat A, Pizard A, Breit A, et al. (2001). "Determination of bradykinin B2 receptor in vivo phosphorylation sites and their role in receptor function.". J. Biol. Chem. 276 (44): 40431–40. doi:10.1074/jbc.M107024200. PMID 11517230.  
  • Willets JM, Challiss RA, Nahorski SR (2002). "Endogenous G protein-coupled receptor kinase 6 Regulates M3 muscarinic acetylcholine receptor phosphorylation and desensitization in human SH-SY5Y neuroblastoma cells.". J. Biol. Chem. 277 (18): 15523–9. doi:10.1074/jbc.M111217200. PMID 11856737.  
  • Grange-Midroit M, García-Sevilla JA, Ferrer-Alcón M, et al. (2002). "G protein-coupled receptor kinases, beta-arrestin-2 and associated regulatory proteins in the human brain: postmortem changes, effect of age and subcellular distribution.". Brain Res. Mol. Brain Res. 101 (1-2): 39–51. doi:10.1016/S0169-328X(02)00144-4. PMID 12007830.  


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