G-protein coupled receptor kinases

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G-Protein coupled receptor kinases regulate the activity of G-protein coupled receptors by phosphorylating their intracellular domains after their associated G-proteins have been released and activated. The phosphorylated serines and threonine residues act as binding sites for Arrestin proteins which prevent the reassociation of the G-proteins with their receptors, thereby preventing reactivation of the signaling pathway.

G-Protein coupled receptor kinase 1 is rhodopsin kinase. G-Protein coupled receptor kinase 2 is beta-adrenergic receptor kinase-1. G-Protein coupled receptor kinase 4 has been associated with regulation of kidney tubule function. Transgenic mice lacking G-Protein coupled receptor kinase 5 have altered core body temperature. Transgenic mice lacking G-Protein coupled receptor kinase 6 have altered response to leukotriene B4

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