G protein-coupled receptor adaptation mechanisms.

Journal Article (Journal Article;Review)

G protein-coupled receptors (GPCRs) transduce extracellular signals that modulate the activity of a wide variety of biological processes, such as neurotransmission, chemoattraction, cardiac function, olfaction, and vision. However, GPCR signalling desensitizes rapidly as the consequence of receptor phosphorylation. G protein-coupled receptor kinase-mediated receptor phosphorylation promotes the binding of beta-arrestin proteins, which not only uncouple GPCRs from their cognate heterotrimeric G protein, but also target them for endocytosis. The sequestration (endocytosis) of desensitized GPCRs to endosomes is required for their dephosphorylation and subsequent resensitization to their pre-ligand exposed state. This review concentrates on the mechanisms underlying GPCR desensitization and resensitization.

Full Text

Duke Authors

Cited Authors

  • Ferguson, SS; Caron, MG

Published Date

  • April 1998

Published In

Volume / Issue

  • 9 / 2

Start / End Page

  • 119 - 127

PubMed ID

  • 9599406

International Standard Serial Number (ISSN)

  • 1084-9521

Digital Object Identifier (DOI)

  • 10.1006/scdb.1997.0216


  • eng

Conference Location

  • England