Overview:

GRK2 or ADRBK1 is a ubiquitous cytosolic enzyme that specifically phosphorylates the activated form of the beta-adrenergic and related G protein-coupled receptors. GRK2 phosphorylates the beta-2-adrenergic receptor and appears to mediate agonist-specific desensitization. Abnormal coupling of beta-adrenergic receptor to G protein is involved in the pathogenesis of the failing heart (1). RAF kinase inhibitor protein RKIP is a physiologic inhibitor of GRK2 (2). After stimulation of G protein-coupled receptors, RKIP dissociates from its known target, RAF1 to associate with GRK2 and block its activity.

Gene Aliases:

ADRBK1; BARK1; BETA-ARK1, FLJ16718

Genbank Number:

NM_001619

References:

1. Rockman, H. A. et al: Expression of a beta-adrenergic receptor kinase 1 inhibitor prevents the development of myocardial failure in gene-targeted mice. Proc. Nat. Acad. Sci. 95: 7000-7005, 1998.

2. Lorenz, K. et al: Protein kinase C switches the Raf kinase inhibitor from Raf-1 to GRK-2. Nature 426: 574-579, 2003.