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Recent developments in biased agonism.

Publication ,  Journal Article
Wisler, JW; Xiao, K; Thomsen, ARB; Lefkowitz, RJ
Published in: Curr Opin Cell Biol
April 2014

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.

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Published In

Curr Opin Cell Biol

DOI

EISSN

1879-0410

Publication Date

April 2014

Volume

27

Start / End Page

18 / 24

Location

England

Related Subject Headings

  • Signal Transduction
  • Receptors, G-Protein-Coupled
  • Protein Conformation
  • Ligands
  • Humans
  • Developmental Biology
  • Biophysical Phenomena
  • Animals
  • 3101 Biochemistry and cell biology
  • 0601 Biochemistry and Cell Biology
 

Citation

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Wisler, J. W., Xiao, K., Thomsen, A. R. B., & Lefkowitz, R. J. (2014). Recent developments in biased agonism. Curr Opin Cell Biol, 27, 18–24. https://doi.org/10.1016/j.ceb.2013.10.008
Wisler, James W., Kunhong Xiao, Alex R. B. Thomsen, and Robert J. Lefkowitz. “Recent developments in biased agonism.Curr Opin Cell Biol 27 (April 2014): 18–24. https://doi.org/10.1016/j.ceb.2013.10.008.
Wisler JW, Xiao K, Thomsen ARB, Lefkowitz RJ. Recent developments in biased agonism. Curr Opin Cell Biol. 2014 Apr;27:18–24.
Wisler, James W., et al. “Recent developments in biased agonism.Curr Opin Cell Biol, vol. 27, Apr. 2014, pp. 18–24. Pubmed, doi:10.1016/j.ceb.2013.10.008.
Wisler JW, Xiao K, Thomsen ARB, Lefkowitz RJ. Recent developments in biased agonism. Curr Opin Cell Biol. 2014 Apr;27:18–24.
Journal cover image

Published In

Curr Opin Cell Biol

DOI

EISSN

1879-0410

Publication Date

April 2014

Volume

27

Start / End Page

18 / 24

Location

England

Related Subject Headings

  • Signal Transduction
  • Receptors, G-Protein-Coupled
  • Protein Conformation
  • Ligands
  • Humans
  • Developmental Biology
  • Biophysical Phenomena
  • Animals
  • 3101 Biochemistry and cell biology
  • 0601 Biochemistry and Cell Biology