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G protein-coupled receptor kinases (GRKs)


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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.


The Kinome image shown here was obtained from Chartier et al. (2013, <a href='' target='_blank'>Figure 4</a>) <a href='' target='_blank'></a> and has been annotated to show the kinases that are targeted by currently approved kinase inhibitor drugs (last updated in April 2018).


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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.

How to cite this family page

Database page citation:

G protein-coupled receptor kinases (GRKs). Accessed on 17/10/2019. IUPHAR/BPS Guide to PHARMACOLOGY,

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Fabbro D, Kelly E, Marrion NV, Peters JA, Faccenda E, Harding SD, Pawson AJ, Sharman JL, Southan C, Davies JA; CGTP Collaborators. (2017) The Concise Guide to PHARMACOLOGY 2017/18: Enzymes. Br J Pharmacol. 174 Suppl 1: S272-S359.