Gene:
adrenergic, beta, receptor kinase 1
Gene ID:
196870
Symbol:
ADRBK1
Species:
1000
Description:
Beta-adrenergic receptor kinase (ADRBK1) phosphorylates the beta-2-adrenergic receptor and appears to mediate agonist-specific desensitization observed at high agonist concentrations. ADRBK1 is an ubiquitous cytosolic enzyme that specifically phosphorylates the activated form of the beta-adrenergic and related G-protein-coupled receptors. The ADRBK1 gene spans approximately 23 kb and is composed of 21 exons. 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 the beta-AR kinase (beta-ARK1), 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.