G-protein coupled receptor kinases

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G-Protein coupled receptor kinases (GRKs), 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.

[edit] Types

Name	Notes	OMIM	Gene
G-protein coupled receptor kinase 1	#1 is rhodopsin kinase	180381	GRK1
G-protein coupled receptor kinase 2 (BARK1)	#2 is beta adrenergic receptor kinase-1	109635	ADRBK1
G-protein coupled receptor kinase 3 (BARK2)	beta adrenergic receptor kinase-2	109636	ADRBK2
G-protein coupled receptor kinase 4	#4 has been associated with regulation of kidney tubule function	137026	GRK4
G-protein coupled receptor kinase 5	Transgenic mice lacking #5 have altered core body temperature	600870	GRK5
G-protein coupled receptor kinase 6	Transgenic mice lacking #6 have altered response to leukotriene B4	600869	GRK6

[edit] External links

• Enzyme classification: EC 2.7.11.16

v • d • e Kinases: Serine/threonine-specific protein kinases (primarily EC 2.7.11) 2.7.11 Pyruvate dehydrogenase kinase - Protein kinase A - Protein kinase G Protein kinase C (Protein kinase Mζ) G-protein coupled receptor kinases (Rhodopsin, Beta adrenergic receptor) Ca2+/calmodulin-dependent (Elongation factor 2 kinase, Myosin light-chain) Phosphorylase - Cyclin-dependent Mitogen-activated (Extracellular signal-regulated, C-Jun N-terminal (MAPK8, MAPK9), P38 mitogen-activated protein) MAP3K - GSK-3 - AMP-activated 2.7.12 MAP2K (1, 2, 3, 4, 5, 6, 7) 2.7.1.37, or unknown Anti-Mullerian hormone receptor - Ataxia telangiectasia mutated - Aurora (A, B) - Mammalian target of rapamycin - Bone morphogenetic protein receptors (1, 2) - CDKL5 - c-Raf - EIF-2 - Ribosomal s6 - Protein kinase B - PDK1