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G protein-coupled receptor kinases, epitomized by βARK, are involved in the rapid phosphorylation and desensitization of GPCR. Classically, high concentrations of β2-adrenoceptor agonists binding to the receptor lead to the consequent activation and dissociation of the heterotrimeric G protein Gs. Gαs activates adenylyl cyclase activity, while Gβγ subunits perform other functions, one of which is to recruit βARK to phosphorylate serine/threonine residues in the cytoplasmic tail of the β2-adrenoceptor. The phosphorylated receptor binds, with high affinity, a member of the arrestin family (ENSFM00250000000572), which prevents further signalling through the G protein (uncoupling) and may allow interaction with scaffolding proteins, such as clathrin, with the possible consequence of internalization and/or degradation.
Database page citation:
G protein-coupled receptor kinases (GRKs). Accessed on 28/03/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=283.
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Fabbro D, Kelly E, Marrion N, Peters JA, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Southan C, Davies JA and CGTP Collaborators (2015) The Concise Guide to PHARMACOLOGY 2015/16: Enzymes. Br J Pharmacol. 172: 6024-6109.