GRK2: multiple roles beyond G protein-coupled receptor desensitization.


Journal Article (Review)

G protein-coupled receptor kinases (GRKs) regulate numerous G protein-coupled receptors (GPCRs) by phosphorylating the intracellular domain of the active receptor, resulting in receptor desensitization and internalization. GRKs also regulate GPCR trafficking in a phosphorylation-independent manner via direct protein-protein interactions. Emerging evidence suggests that GRK2, the most widely studied member of this family of kinases, modulates multiple cellular responses in various physiological contexts by either phosphorylating non-receptor substrates or interacting directly with signaling molecules. In this review, we discuss traditional and newly discovered roles of GRK2 in receptor internalization and signaling as well as its impact on non-receptor substrates. We also discuss novel exciting roles of GRK2 in the regulation of dopamine receptor signaling and in the activation and trafficking of the atypical GPCR, Smoothened (Smo).

Full Text

Duke Authors

Cited Authors

  • Evron, T; Daigle, TL; Caron, MG

Published Date

  • March 2012

Published In

Volume / Issue

  • 33 / 3

Start / End Page

  • 154 - 164

PubMed ID

  • 22277298

Pubmed Central ID

  • 22277298

Electronic International Standard Serial Number (EISSN)

  • 1873-3735

Digital Object Identifier (DOI)

  • 10.1016/


  • eng

Conference Location

  • England