G-protein-coupled receptor kinase

G-protein-coupled receptor kinases (GRKs) are a family of enzymes that catalyze the phosphorylation of threonine or serine residues on G-protein-coupled receptors. Characteristically, GRKs only phosphorylate the ligand-activated form of the receptors. Phosphorylation by GRKs usually leads to impaired receptor/G-protein coupling. 

G-protein-coupled Receptor Kinases (GRKs) G-protein-coupled Receptors... 

Homologous desensitization is a form of desensitization which is mediated by agonist-induced activation of the same receptor. G-protein-coupled receptor kinases (GRKs) and arrestins are involved in this process, which leads to an uncoupling of the receptor from its G protein. 

G-protein-coupled Receptor Kinases (GRKs) G-protein-coupled Receptors G-proteins and Wnt Signaling Granulocyte-CSF (G-CSF) Granulocyte-macrophage-CSF (GM-CSF)... 

Premont RT, Gainetdinov RR (2007) Physiological roles of G protein-coupled receptor kinases and arrestins. Annu Rev Physiol 69 511-534... 

Ping YF, Yao XH, Chen JH, Liu H, Chen DL, Zhou XD, Wang JM, Bian XW (2007) The anticancer compound Nordy inhibits CXCR4-mediated production of IL-8 and VEGF by malignant human glioma cells. J Neurooncol 84 21-29 Pitcher JA, Freedman NJ, Lefkowitz RJ (1998) G protein-coupled receptor kinases. Annu Rev Biochem 67 653-692... 

Pei G, Kieffer BL, Lefkowitz RJ et al. Agonist-dependent phosphorylation of the mouse K-opioid receptor involvement of G protein-coupled receptor kinases but not protein kinase C. Mol Pharmacol 1995 48 173-177. 

Wang HL. A cluster of Ser/Thr residues at the C-terminus of mu-opioid receptor is required for G protein-coupled receptor kinase 2-mediated desensitization. Neuropharmacology 2000 353—363. 

Mundell, S. J., Pula, G., Carswell, K., Roberts, P. J., and Kelly, E. (2003) Agonist-induced internalization of metabotropic glutamate receptor 1A structural determinants for protein kinase C- and G protein-coupled receptor kinase-mediated internalization../. Neurochem. 84,294-304. 

Dale, L. B., Bhattacharya, M., Anborgh, P. H., Murdoch, B., Bhatia, M., Nakanishi, S., and Ferguson, S. S. (2000) G protein-coupled receptor kinase-mediated desensitization of metabotropic glutamate receptor 1A protects against cell death. J. Biol. Chem. 275, 38213-38220. 

Sallese, M., Salvatore, L., D Urbano, E., et al. (2000) The G protein-coupled receptor kinase GRK4 mediates homologous desensitization of metabotropic glutamate receptor 1. FASEB J. 14, 2569-2580. 

Keywords Accessory proteins G protein-coupled receptor G protein-coupled receptor kinases hypertension pharmacogenomics signaling. 

G protein-coupled receptor kinase 1, rhodopsin kinase RHOK/ GRKl) 13q34 Exon 5 deletion Oguchi disease, reces-sively inherited stationary night blindness Impairment of GRKl-mediated desensitization of rhodopsin (189-191)... 

Diviani, D., Lattion, A. L., and Cotecchia, S. (1997) Characterization of the phosphorylation sites involved in G protein- coupled receptor kinase- and protein kinase C-mediated desensitization of the alphalB-adrenergic receptor. J. Biol. Chem. 272, 28712-28719. 

Tsuga, H., Kameyama, K., Haga, T., Honma, T., Lameh, J., and Sadee, W. (1998) Internalization and down-regulation of human muscarinic acetylcholine receptor m2 subtypes. Role of third intracellular m2 loop and G protein- coupled receptor kinase 2. J. Biol. Chem. 273, 5323-5330. 

Tiberi, M., Nash, S. R., Bertrand, L., Lefkowitz, R. J., and Caron, M. G. (1996) Differential regulation of dopamine receptor responsiveness by various G protein-coupled receptor kinases. J. Biol. Chem. 271, 3771-3778. 

Guo, J., Wu, Y., Zhang, W., Zhao, L, Devi, L. A., Pei, G., and Ma, L. (2000) Identification of G protein-coupled receptor kinase 2 phosphorylation sites responsible for agonist-stimn-lated delta-opioid receptor phosphorylation. Mol. Pharmacol. 58, 1050-1056. 

Oppermann, M., Diverse-Pierluissi, M., Drazner, M. H., et al. (1996) Monoclonal antibodies reveal receptor specificity among G-protein-coupled receptor kinases. Proc. Natl. Acad. Sci. U. S. A. 93, 7649-7654. 

Loudon, R. P., and Benovic, J. L. (1994) Expression, purification, and characterization of the G protein-coupled receptor kinase GRK6. J. Biol. Chem. 269, 22691-22697. 

Seibold, A., January, B. G., Friedman, J., Hipkin, R. W., and Clark, R. B. (1998) Desensitization of beta2-adrenergic receptors with mutations of the proposed G protein-coupled receptor kinase phosphorylation sites. J. Biol. Chem. 273, 7637-7642. 

Delmas P, Abogadie FC, Milligan G, Buckley NJ, Brown DA (1999) Py dimers derived from Go and Gj proteins contribute different components of adrenergic inhibiton of Ca channels in rat sympathetic neurons. J Physiol 518 23-36 Diverse-Pierluissi M, Inglese J, Stoffel RH, Lefkowitz RJ, Dunlap K (1996) G protein-coupled receptor kinase mediates desensitization of norepinephrine-induced Ca channel inhibition. Neuron 16 579-585 Docherty JR (1998) Subtypes of fimctional ap and a2-adrenoceptors. Eur J Pharmacol 361 1-15... 

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