G protein-coupled receptor kinases (GRKs) are important regulators of G protein-coupled receptors(GPCRs). GRK2 (83 kDa), one of six members of this family that have been identified, is ubiquitously expressed in mammals. After binding to their ligand and interacting with heterotrimeric G proteins, GPCRs (e.g., a2-adrenergic receptor) are phosphorylated by GRKs. Internalization of the GPCRs, regulated by beta-arrestin-1, leads to activation of the Ras - Raf - ERK1 and 2 signaling pathway. GRK2 activity is tightly controlled by different mechanisms including phosphorylation by kinases such as PKC, Src and ERK1 and 2, as well as interaction with various proteins. ERK phosphorylates and thus inactivates GRK2 on serine 670 in a negative feedback mechanism.
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Protein Aliases: adrenergic beta receptor kinase 1; adrenergic receptor kinase, beta 1; adrenergic, beta, receptor kinase 1; Beta-adrenergic receptor kinase 1; beta-adrenergic receptor kinase 1 beta ARK1; beta-AR kinase-1; Beta-ARK-1; EC 126.96.36.199; G-protein coupled receptor kinase 2; G-protein-coupled receptor kinase 2; grk 2
Gene Aliases: Adrbk-1; ADRBK1; BARK; Bark-1; BARK1; beta ARK; BETA-ARK1; betaARK1; GRK-2; GRK2