GRK5 Antibody – Rabbit Polyclonal

This gene encodes a member of the guanine nucleotide-binding protein (G protein)-coupled receptor kinase subfamily of the Ser/Thr protein kinase family. The protein phosphorylates the activated forms of G protein-coupled receptors thus initiating their deactivation. It has also been shown to play a role in regulating the motility of polymorphonuclear leukocytes (PMNs). [provided by RefSeq, Jul 2008]

GRK5: Serine/threonine kinase that phosphorylates preferentially the activated forms of a variety of G-protein- coupled receptors (GPCRs). Such receptor phosphorylation initiates beta-arrestin-mediated receptor desensitization, internalization, and signaling events leading to their down-regulation. Phosphorylates a variety of GPCRs, including adrenergic receptors, muscarinic acetylcholine receptors (more specifically Gi-coupled M2/M4 subtypes), dopamine receptors and opioid receptors. In addition to GPCRs, also phosphorylates various substrates: Hsc70- interacting protein/ST13, TP53/p53, HDAC5, and arrestin-1/ARRB1. Phosphorylation of ARRB1 by GRK5 inhibits G-protein independent MAPK1/MAPK3 signaling downstream of 5HT4-receptors. Phosphorylation of HDAC5, a repressor of myocyte enhancer factor 2 (MEF2) leading to nuclear export of HDAC5 and allowing MEF2- mediated transcription. Phosphorylation of TP53/p53, a crucial tumor suppressor, inhibits TP53/p53-mediated apoptosis. Phosphorylation of ST13 regulates internalization of the chemokine receptor. Phosphorylates rhodopsin (RHO) (in vitro) and a non G- protein-coupled receptor, LRP6 during Wnt signaling (in vitro). Belongs to the protein kinase superfamily. AGC Ser/Thr protein kinase family. GPRK subfamily.

Protein type: Kinase, protein; Protein kinase, AGC; EC 2.7.11.16; Protein kinase, Ser/Thr (non-receptor); AGC group; GRK family; GRK subfamily

Chromosomal Location of Human Ortholog: 10q26.11

Cellular Component: cytoplasm; focal adhesion; nuclear membrane; nucleus; plasma membrane

Molecular Function: ATP binding; beta-adrenergic receptor kinase activity; G-protein coupled receptor kinase activity; phospholipid binding; protein binding; protein kinase C binding; protein serine/threonine kinase activity

Biological Process: apoptosis; desensitization of G-protein coupled receptor protein signaling pathway; fat cell differentiation; G-protein signaling, coupled to cAMP nucleotide second messenger; negative regulation of apoptosis; positive regulation of cell proliferation; protein amino acid autophosphorylation; regulation of cell cycle; regulation of G-protein coupled receptor protein signaling pathway; response to drug; tachykinin signaling pathway; Wnt receptor signaling pathway