G protein-coupled receptor kinases.
Journal Article (Journal Article;Review)
G protein-coupled receptor kinases (GRKs) constitute a family of six mammalian serine/threonine protein kinases that phosphorylate agonist-bound, or activated, G protein-coupled receptors (GPCRs) as their primary substrates. GRK-mediated receptor phosphorylation rapidly initiates profound impairment of receptor signaling, or desensitization. This review focuses on the regulation of GRK activity by a variety of allosteric and other factors: agonist-stimulated GPCRs, beta gamma subunits of heterotrimeric GTP-binding proteins, phospholipid cofactors, the calcium-binding proteins calmodulin and recoverin, posttranslational isoprenylation and palmitoylation, autophosphorylation, and protein kinase C-mediated GRK phosphorylation. Studies employing recombinant, purified proteins, cell culture, and transgenic animal models attest to the general importance of GRKs in regulating a vast array of GPCRs both in vitro and in vivo.
Full Text
Duke Authors
Cited Authors
- Pitcher, JA; Freedman, NJ; Lefkowitz, RJ
Published Date
- January 1, 1998
Published In
Volume / Issue
- 67 /
Start / End Page
- 653 - 692
PubMed ID
- 9759500
International Standard Serial Number (ISSN)
- 0066-4154
Digital Object Identifier (DOI)
- 10.1146/annurev.biochem.67.1.653
Language
- eng
Conference Location
- United States