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Overview
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.
How to cite this family page
Database page citation:
G protein-coupled receptor kinases (GRKs). Accessed on 09/04/2026. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=283.
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Fabbro D, Gibb AJ, Kelly E, Mathie AA, Peach CJ, Veale EL, Armstrong JF, Faccenda E, Harding SD, Southan C, Davies JA et al. (2025) The Concise Guide to PHARMACOLOGY 2025/26: Enzymes. Br J Pharmacol. 182: S307-S403.
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Loss-of-function mutations in RHOK or retinal and pineal gland arrestin (SAG, P10523) are associated with Oguchi disease (OMIM: 181301), a form of congenital stationary night blindness.