[G-protein-coupled receptors targeting: the allosteric approach]

Med Sci (Paris). 2012 Oct;28(10):845-51. doi: 10.1051/medsci/20122810012. Epub 2012 Oct 12.
[Article in French]


G-protein-coupled receptors (GPCR) are a major family of drug targets. Essentially all drugs targeting these receptors on the market compete with the endogenous ligand (agonists or antagonists) for binding the receptor. Recently, non-competitive compounds binding to distinct sites from the cognate ligand were documented in various classes of these receptors. These compounds, called allosteric modulators, generally endowed of a better selectivity are able to modulate specifically the endogenous signaling of the receptor. To better understand the promising potential of this class of GPCRs targeting compounds, this review highlights the properties of allosteric modulators, the strategies used to identify them and the challenges associated with the development of these compounds.

Publication types

  • English Abstract
  • Review

MeSH terms

  • Allosteric Regulation
  • Allosteric Site / physiology*
  • Animals
  • Drug Design*
  • High-Throughput Screening Assays
  • Humans
  • Models, Biological
  • Molecular Targeted Therapy* / methods
  • Receptors, G-Protein-Coupled* / agonists
  • Receptors, G-Protein-Coupled* / antagonists & inhibitors
  • Receptors, G-Protein-Coupled* / metabolism


  • Receptors, G-Protein-Coupled