Recent developments in biased agonism.

Published

Journal Article (Review)

The classic paradigm of G protein-coupled receptor (GPCR) activation was based on the understanding that agonist binding to a receptor induces or stabilizes a conformational change to an 'active' conformation. In the past decade, however, it has been appreciated that ligands can induce distinct 'active' receptor conformations with unique downstream functional signaling profiles. Building on the initial recognition of the existence of such 'biased ligands', recent years have witnessed significant developments in several areas of GPCR biology. These include increased understanding of structural and biophysical mechanisms underlying biased agonism, improvements in characterization and quantification of ligand efficacy, as well as clinical development of these novel ligands. Here we review recent major developments in these areas over the past several years.

Full Text

Duke Authors

Cited Authors

  • Wisler, JW; Xiao, K; Thomsen, ARB; Lefkowitz, RJ

Published Date

  • April 2014

Published In

Volume / Issue

  • 27 /

Start / End Page

  • 18 - 24

PubMed ID

  • 24680426

Pubmed Central ID

  • 24680426

Electronic International Standard Serial Number (EISSN)

  • 1879-0410

Digital Object Identifier (DOI)

  • 10.1016/j.ceb.2013.10.008

Language

  • eng

Conference Location

  • England