[Beta-adrenergic receptor kinase 1 (ADRBK1), encoded by the ADRBK1 gene, phosphorylates the beta-2-adrenergic receptor and mediates agonist-specific desensitization observed at high agonist concentrations. ADRBK1, an ubiquitous cytosolic enzyme, translocates from the cytosol to the plasma membrane upon agonist stimulation and specifically phosphorylates the activated form of the beta-adrenergic and related G-protein-coupled receptors. Heart failure is accompanied by severely impaired beta-adrenergic receptor (beta-AR) function. An important mechanism for the rapid desensitization of beta-AR function is agonist-stimulated receptor phosphorylation by ADRBK1, an enzyme known to be elevated in failing human heart tissue. Abnormal coupling of beta-adrenergic receptor to G protein is involved in the pathogenesis of the failing heart. Inhibition of ADRBK1 is a novel mode of therapy. (From LocusLink) ( NCI )]
UMLS (NCI) C0753114BARK1
Beta-Adrenergic Receptor Kinase 1
BETA-ARK1
Beta-ARK-1
EC 2.7.1.126
G-Protein Coupled Receptor Kinase 2
GRK2
- Amino Acid, Peptide, or Protein
- Enzyme
- Receptor