A cellular perspective of bias at G protein-coupled receptors

Thomas J. Fernandez, Monica De Maria, Braden T. Lobingier

Research output: Contribution to journalReview articlepeer-review

4 Scopus citations

Abstract

G protein-coupled receptors (GPCRs) modulate cell function over short- and long-term timescales. GPCR signaling depends on biochemical parameters that define the what, when, and where of receptor function: what proteins mediate and regulate receptor signaling, where within the cell these interactions occur, and how long these interactions persist. These parameters can vary significantly depending on the activating ligand. Collectivity, differential agonist activity at a GPCR is called bias or functional selectivity. Here we review agonist bias at GPCRs with a focus on ligands that show dramatically different cellular responses from their unbiased counterparts.

Original languageEnglish (US)
Pages (from-to)1345-1354
Number of pages10
JournalProtein Science
Volume29
Issue number6
DOIs
StatePublished - Jun 1 2020

Keywords

  • GPCR
  • agonist bias
  • desensitization
  • signaling

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology

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