G Protein-coupled Receptor Biased Agonism.

Journal Article (Journal Article;Review)

G protein-coupled receptors are the largest family of targets for current therapeutics. The classic model of their activation was binary, where agonist binding induced an active conformation and subsequent downstream signaling. Subsequently, the revised concept of biased agonism emerged, where different ligands at the same G protein-coupled receptor selectively activate one downstream pathway versus another. Advances in understanding the mechanism of biased agonism have led to the development of novel ligands, which have the potential for improved therapeutic and safety profiles. In this review, we summarize the theory and most recent breakthroughs in understanding biased signaling, examine recent laboratory investigations concerning biased ligands across different organ systems, and discuss the promising clinical applications of biased agonism.

Full Text

Duke Authors

Cited Authors

  • Hodavance, SY; Gareri, C; Torok, RD; Rockman, HA

Published Date

  • March 2016

Published In

Volume / Issue

  • 67 / 3

Start / End Page

  • 193 - 202

PubMed ID

  • 26751266

Pubmed Central ID

  • PMC4783281

Electronic International Standard Serial Number (EISSN)

  • 1533-4023

Digital Object Identifier (DOI)

  • 10.1097/FJC.0000000000000356


  • eng

Conference Location

  • United States