Feedback regulation of G protein-coupled receptor signaling by GRKs and arrestins.


Journal Article (Review)

GPCRs are ubiquitous in mammalian cells and present intricate mechanisms for cellular signaling and communication. Mechanistically, GPCR signaling was identified to occur vectorially through heterotrimeric G proteins that are negatively regulated by GRK and arrestin effectors. Emerging evidence highlights additional roles for GRK and Arrestin partners, and establishes the existence of interconnected feedback pathways that collectively define GPCR signaling. GPCRs influence cellular dynamics and can mediate pathologic development, such as cancer and cardiovascular remolding. Hence, a better understanding of their overall signal regulation is of great translational interest and research continues to exploit the pharmacologic potential for modulating their activity.

Full Text

Cited Authors

  • Black, JB; Premont, RT; Daaka, Y

Published Date

  • February 2016

Published In

Volume / Issue

  • 50 /

Start / End Page

  • 95 - 104

PubMed ID

  • 26773211

Pubmed Central ID

  • 26773211

Electronic International Standard Serial Number (EISSN)

  • 1096-3634

International Standard Serial Number (ISSN)

  • 1084-9521

Digital Object Identifier (DOI)

  • 10.1016/j.semcdb.2015.12.015


  • eng