Beta-adrenergic-receptor kinase

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.

References

• Benovic JL, Mayor F Jr, Staniszewski C, Lefkowitz RJ, Caron MG "Purification and characterization of the beta-adrenergic receptor kinase". J. Biol. Chem. 262 9026–32.
• Kim CM, Dion SB, Onorato JJ, Benovic JL "Expression and characterization of two beta-adrenergic receptor kinase isoforms using the baculovirus expression system". Receptor. 3 39–55.
• A, Ungerer M "Characterization and inhibition of beta-adrenergic receptor kinase in intact myocytes". Cardiovasc. Res. 35 324–33.
• Ferguson SS, Menard L, Barak LS, Koch WJ, Colapietro AM, Caron MG "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.
• Willets JM, Challiss RA, Nahorski SR "Non-visual GRKs: are we seeing the whole picture?". Trends. Pharmacol. Sci. 24 626–33.

External links

The CAS registry number for this enzyme class is .

Gene Ontology (GO) codes