G protein coupled receptor kinase 6


Gene Symbol: G protein coupled receptor kinase 6
Description: G protein-coupled receptor kinase 6
Alias: Gprk6, G protein-coupled receptor kinase 6, g protein-coupled receptor kinase GRK6
Species: rat

Top Publications

  1. Wu N, Song L, Yang X, Wei J, Liu Z. [Effects of Chinese herbal medicine Tianqi Pingchan Granule on G protein-coupled receptor kinase 6 involved in the prevention of levodopa-induced dyskinesia in rats with Parkinson disease]. Zhong Xi Yi Jie He Xue Bao. 2012;10:1018-24 pubmed
    ..01), which was observed by Western blotting. TGPC Granule can increase the expression of GRK6, inhibit the increase of AIM, and reduce the incidence of levodopa-induced dyskinesia in rats with PD. ..
  2. Beaulieu J, Gainetdinov R. The physiology, signaling, and pharmacology of dopamine receptors. Pharmacol Rev. 2011;63:182-217 pubmed publisher
  3. Ahmed M, Berthet A, Bychkov E, Porras G, Li Q, Bioulac B, et al. Lentiviral overexpression of GRK6 alleviates L-dopa-induced dyskinesia in experimental Parkinson's disease. Sci Transl Med. 2010;2:28ra28 pubmed publisher
  4. Tarrant T, Rampersad R, Esserman D, Rothlein L, Liu P, Premont R, et al. Granulocyte chemotaxis and disease expression are differentially regulated by GRK subtype in an acute inflammatory arthritis model (K/BxN). Clin Immunol. 2008;129:115-22 pubmed publisher
    ..GRK6 and -2, but not GRK5, are involved in the pathogenesis of acute arthritis in the K/BxN model. In particular, GRK6 may dampen inflammatory responses by regulating granulocyte trafficking toward chemoattractants. ..
  5. Hillhouse E, Grammatopoulos D. The molecular mechanisms underlying the regulation of the biological activity of corticotropin-releasing hormone receptors: implications for physiology and pathophysiology. Endocr Rev. 2006;27:260-86 pubmed
    ..The type of activating agonist, receptor, and target cell appears to play a major role in determining the overall signaling and biological responses in health and disease. ..
  6. Zhou Y, Li R, Li M, Liu X, Zhu H, Ju Z, et al. Overexpression of GRK6 attenuates neuropathic pain via suppression of CXCR2 in rat dorsal root ganglion. Mol Pain. 2016;12: pubmed publisher
  7. Oda Y, Tadokoro S, Takase M, Kanahara N, Watanabe H, Shirayama Y, et al. G protein-coupled receptor kinase 6/β-arrestin 2 system in a rat model of dopamine supersensitivity psychosis. J Psychopharmacol. 2015;29:1308-13 pubmed publisher
    ..Our results suggest that alterations of the GRK6 and ARRB2 system could induce both DRD2 up-regulation and impairment of the dopamine signaling pathway, resulting potentially in the development of DSP. ..
  8. Willets J, Nelson C, Nahorski S, Challiss R. The regulation of M1 muscarinic acetylcholine receptor desensitization by synaptic activity in cultured hippocampal neurons. J Neurochem. 2007;103:2268-80 pubmed
    ..Taken together these data suggest that the level of synaptic activity may determine the different kinases recruited to regulate M1 mACh receptor desensitization in neurons. ..
  9. Miyoshi T, Otsuka F, Shimasaki S. GRK-6 mediates FSH action synergistically enhanced by estrogen and the oocyte in rat granulosa cells. Biochem Biophys Res Commun. 2013;434:401-6 pubmed publisher
    ..Consequently, these findings strongly suggest that GRK-6 is involved in the mechanism by which estrogen and oocytes synergistically augment FSH activity in granulosa cells. ..

More Information


  1. Lombardi M, Kavelaars A, Schedlowski M, Bijlsma J, Okihara K, van de Pol M, et al. Decreased expression and activity of G-protein-coupled receptor kinases in peripheral blood mononuclear cells of patients with rheumatoid arthritis. FASEB J. 1999;13:715-25 pubmed
  2. Zhou Y, Huang X, Wu H, Xu Y, Tao T, Xu G, et al. Decreased expression and role of GRK6 in spinal cord of rats after chronic constriction injury. Neurochem Res. 2013;38:2168-79 pubmed publisher
    ..All the data indicated that down-regulation of neuronal GRK6 expression induced by cytokine may be a potential mechanism that contributes to increasing neuronal signaling in neuropathic pain. ..
  3. Firsov D, Elalouf J. Molecular cloning of two rat GRK6 splice variants. Am J Physiol. 1997;273:C953-61 pubmed
    ..The identification of GRK6b extends the family of GRKs. Further studies will be required to establish the tissue and subcellular distribution of this protein and to delineate its physiological role...
  4. Sun B, Gao Y, Lou D, Wu X, Wei H, Wen H, et al. Expression of G-protein-coupled receptor kinase 6 (GRK6) after acute spinal cord injury in adult rat. J Mol Histol. 2013;44:259-70 pubmed publisher
    ..These data suggested that GRK6 might be involved in the pathophysiology of SCI. ..
  5. Ahmed M, Bychkov E, Gurevich V, Benovic J, Gurevich E. Altered expression and subcellular distribution of GRK subtypes in the dopamine-depleted rat basal ganglia is not normalized by l-DOPA treatment. J Neurochem. 2008;104:1622-36 pubmed
    ..The data suggest that alterations in the expression and subcellular distribution of arrestins and GRKs contribute to pathophysiology of Parkinson's disease. Thus, these proteins may be targets for antiparkinsonian therapy. ..
  6. Hong S, Li H, Becker K, Dawson V, Dawson T. Identification and analysis of plasticity-induced late-response genes. Proc Natl Acad Sci U S A. 2004;101:2145-50 pubmed
    ..Our results provide a molecular dissection of the activity-dependent long-lasting neuronal responses induced by NMDA receptor activation. ..
  7. Baameur F, Morgan D, Yao H, Tran T, Hammitt R, Sabui S, et al. Role for the regulator of G-protein signaling homology domain of G protein-coupled receptor kinases 5 and 6 in beta 2-adrenergic receptor and rhodopsin phosphorylation. Mol Pharmacol. 2010;77:405-15 pubmed publisher
  8. Premont R, Macrae A, Aparicio S, Kendall H, Welch J, Lefkowitz R. The GRK4 subfamily of G protein-coupled receptor kinases. Alternative splicing, gene organization, and sequence conservation. J Biol Chem. 1999;274:29381-9 pubmed
    ..The divergence of individual GRKs at vastly different rates reveals that strikingly different evolutionary pressures apply to the function of the individual GRKs. ..
  9. Simon V, Robin M, Legrand C, Cohen Tannoudji J. Endogenous G protein-coupled receptor kinase 6 triggers homologous beta-adrenergic receptor desensitization in primary uterine smooth muscle cells. Endocrinology. 2003;144:3058-66 pubmed
    ..Conversely, expression of (K215R)GRK5 or (K220R)GRK2 had no effect on beta-adrenergic signaling. These results strongly suggest that endogenous GRK6 mediate homologous beta-AR desensitization in myometrial cells. ..
  10. Sato H, Arawaka S, Hara S, Fukushima S, Koga K, Koyama S, et al. Authentically phosphorylated ?-synuclein at Ser129 accelerates neurodegeneration in a rat model of familial Parkinson's disease. J Neurosci. 2011;31:16884-94 pubmed publisher
  11. Fehr C, Fickova M, Hiemke C, Reuss S, Dahmen N. Molecular cloning of rat G-protein-coupled receptor kinase 6 (GRK6) from brain tissue, and its mRNA expression in different brain regions and peripheral tissues. Brain Res Mol Brain Res. 1997;49:278-82 pubmed
    ..7% identical and 97.9% similar to its human counterpart. mRNA was detectable in all brain areas examined. In addition, GRK6 was expressed in skeletal muscle, small intestine, aorta, liver, heart, lung, thymus, stomach, uterus and kidney. ..
  12. Shenoy S, Lefkowitz R. Angiotensin II-stimulated signaling through G proteins and beta-arrestin. Sci STKE. 2005;2005:cm14 pubmed
  13. Fraga S, Luo Y, Jose P, Zandi Nejad K, Mount D, Soares da Silva P. Dopamine D1-like receptor-mediated inhibition of Cl/HCO3- exchanger activity in rat intestinal epithelial IEC-6 cells is regulated by G protein-coupled receptor kinase 6 (GRK 6). Cell Physiol Biochem. 2006;18:347-60 pubmed
    ..Dopamine D1 receptors in IEC-6 rapidly desensitize to D1-like agonist stimulation and GRK 6, but not GRK 4, appear to be involved in agonist-mediated responsiveness and desensitization. ..