Beta-adrenergic-receptor kinase

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In enzymology, a beta-adrenergic-receptor kinase (EC 2.7.11.15) is an enzyme that catalyzes the chemical reaction:

ATP + [beta-adrenergic receptor] \rightleftharpoons ADP + phospho-[beta-adrenergic receptor]

Thus, the two substrates of this enzyme are ATP and beta-adrenergic receptor, whereas its two products are ADP and phospho-beta-adrenergic receptor.

This enzyme belongs to the family of transferases, specifically those transferring a phosphate group to the sidechain oxygen atom of serine or threonine residues in proteins (protein-serine/threonine kinases). The systematic name of this enzyme class is ATP:[beta-adrenergic receptor] phosphotransferase. Other names in common use include ATP:beta-adrenergic-receptor phosphotransferase, [beta-adrenergic-receptor] kinase, beta-adrenergic receptor-specific kinase, beta-AR kinase, beta-ARK, beta-ARK 1, beta-ARK 2, beta-receptor kinase, GRK2, GRK3, beta-adrenergic-receptor kinase (phosphorylating), beta2ARK, betaARK1, beta-adrenoceptor kinase, beta-adrenoceptor kinase 1, beta-adrenoceptor kinase 2, ADRBK1, BARK1, adrenergic receptor kinase, and STK15. Several compounds are known to inhibit this enzyme, including Zinc, and Digitonin.

[edit] References

  • IUBMB entry for 2.7.11.15
  • BRENDA references for 2.7.11.15 (Recommended.)
  • PubMed references for 2.7.11.15
  • PubMed Central references for 2.7.11.15
  • Google Scholar references for 2.7.11.15
  • Benovic JL, Mayor F Jr, Staniszewski C, Lefkowitz RJ, Caron MG (1987). "Purification and characterization of the beta-adrenergic receptor kinase". J. Biol. Chem. 262: 9026–32. PMID 87250541. 
  • Kim CM, Dion SB, Onorato JJ, Benovic JL (1993). "Expression and characterization of two beta-adrenergic receptor kinase isoforms using the baculovirus expression system". Receptor. 3: 39–55. PMID 8394172. 
  • A, Ungerer M (1997). "Characterization and inhibition of beta-adrenergic receptor kinase in intact myocytes". Cardiovasc. Res. 35: 324–33. PMID 9349395. 
  • Ferguson SS, Menard L, Barak LS, Koch WJ, Colapietro AM, Caron MG (1995). "Role of phosphorylation in agonist-promoted beta 2-adrenergic receptor sequestration. Rescue of a sequestration-defective mutant receptor by beta ARK1". J. Biol. Chem. 270: 24782–9. PMID 7559596. 
  • Willets JM, Challiss RA, Nahorski SR (2003). "Non-visual GRKs: are we seeing the whole picture?". Trends. Pharmacol. Sci. 24: 626–33. PMID 14654303. 

[edit] External links

The CAS registry number for this enzyme class is 102925-39-3.

[edit] Gene Ontology (GO) codes