Allosteric modulators: the new generation of receptor antagonist

Mol Interv. 2004 Aug;4(4):222-9. doi: 10.1124/mi.4.4.6.


Allosteric antagonists modulate the affinity and/or efficacy of agonists for receptors. Although the manner in which this modulation can occur can mimic that of simple competitive antagonists, allosteric antagonists possess unique properties that can present seemingly capricious profiles of antagonism. These unique properties also offer potentially useful patterns for therapeutic utility. This review summarizes methods to detect allosteric antagonism and some special properties of these receptor modulators.

Publication types

  • Review

MeSH terms

  • Allosteric Regulation*
  • Humans
  • Protein Binding
  • Receptors, Cell Surface / antagonists & inhibitors*
  • Receptors, Cell Surface / metabolism


  • Receptors, Cell Surface