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GRK2 a ubiquitous protein kinase of the GRK family. Phosphorylates the beta-2-adrenergic receptor and related G-protein-coupled receptors. Appears to mediate agonist-specific desensitization observed at high agonist concentrations. Expression level is consistently elevated in chronic human heart failure. Mouse models of severe heart failure have been used to demonstrate that inhibition of BARK1 with a peptide inhibitor is sufficient to increase mean survival, reduce dialation and improve cardiac function. Note: This description may include information from UniProtKB.
Protein type: AGC group; BARK subfamily; EC; GRK family; Kinase, protein; Protein kinase, AGC; Protein kinase, Ser/Thr (non-receptor)
Chromosomal Location of Human Ortholog: 19 A|19 3.98 cM
Cellular Component: apical plasma membrane; axon; basolateral plasma membrane; caveola; cytoplasm; dendritic shaft; dendritic spine; membrane; synapse
Molecular Function: beta-adrenergic receptor kinase activity; Edg-2 lysophosphatidic acid receptor binding; G-protein coupled receptor kinase activity; protein binding; protein kinase activity; protein serine/threonine kinase activity
Biological Process: cardiac muscle contraction; desensitization of G-protein coupled receptor protein signaling pathway; entry of virus into host cell; follicle-stimulating hormone signaling pathway; G-protein coupled receptor protein signaling pathway; heart development; negative regulation of G-protein coupled receptor protein signaling pathway; negative regulation of striated muscle contraction; negative regulation of the force of heart contraction by chemical signal; peptidyl-serine phosphorylation; peptidyl-threonine phosphorylation; positive regulation of catecholamine secretion; protein amino acid phosphorylation; receptor internalization; regulation of the force of heart contraction; response to organic cyclic substance; response to oxidative stress; tachykinin signaling pathway; viral genome replication
Reference #:  Q99MK8 (UniProtKB)
Alt. Names/Synonyms: Adrbk-1; Adrbk1; adrenergic receptor kinase, beta 1; ARBK1; Bark-1; beta ARK; beta ARK1; Beta-adrenergic receptor kinase 1; beta-adrenergic receptor kinase-1; beta-AR kinase-1; Beta-ARK-1; betaARK1; G-protein-coupled receptor kinase 2; Grk2
Gene Symbols: Adrbk1
Molecular weight: 79,639 Da
Basal Isoelectric point: 6.89  Predict pI for various phosphorylation states
CST Pathways:  GPCR Signaling to MAPKs
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