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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.
Gene Name: | adrenergic, beta, receptor kinase 1 |
Family/Subfamily: | Protein Kinase , GPRK |
Synonyms: | ADRBK1, BARK1, Beta-ARK-1, BETA-ARK1, BARK, Betaark1, GRK2 |
Target Sequences: | NM_001619 NP_001610.2 P25098 |
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