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.
ADRBK1; BARK1; BETA-ARK1, FLJ16718
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.
Sample Kinase Activity Plot. For specific information on a given lot, see related technical data sheet.
Sample Purity Data. For specific information on a given lot, see related technical data sheet.
Storage, Stability and Shipping:
Store product at –70oC. For optimal storage, aliquot target into smaller quantities after centrifugation and store at recommended temperature. For most favorable performance, avoid repeated handling and multiple freeze/thaw cycles.
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Angiogenesis, Cancer, Cardiovascular Disease, ERK/MAPK Pathway, Invasion/Metastasis, Metabolic Disorder, Neurobiology, Ser/Thr Kinases