Targeting G protein-coupled receptor kinases (GRKs) to G protein-coupled receptors
- PMID: 33718657
- PMCID: PMC7945687
- DOI: 10.1016/j.coemr.2020.09.002
Targeting G protein-coupled receptor kinases (GRKs) to G protein-coupled receptors
Abstract
G protein-coupled receptors (GPCRs) interact with three protein families following agonist binding: heterotrimeric G proteins, G protein-coupled receptor kinases (GRKs) and arrestins. GRK-mediated phosphorylation of GPCRs promotes arrestin binding to uncouple the receptor from G protein, a process called desensitization, and for many GPCRs, arrestin binding also promotes receptor endocytosis and intracellular signaling. Thus, GRKs play a central role in modulating GPCR signaling and localization. Here we review recent advances in this field which include additional insight into how GRKs target GPCRs and bias signaling, and the development of specific inhibitors to dissect GRK function in model systems.
Keywords: arrestin; cell signaling; desensitization; endocytosis; phosphorylation; protein kinase.
Conflict of interest statement
Declaration of interest The authors declare no competing interests. Declaration of interests: none
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