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


  • eng

Conference Location

  • United States