Allosterism and cannabinoid CB1 receptors: the shape of things to come

Ruth A. Ross

Research output: Contribution to journalLiterature review

72 Citations (Scopus)

Abstract

In 2005, the first evidence was obtained that the cannabinoid CB, receptor contains an allosteric binding site. The site can be recognized by synthetic small molecules, which display a markedly divergent effect on orthosteric ligand affinity versus efficacy; these small molecules are allosteric enhancers of agonist binding affinity and allosteric inhibitors of agonist signalling efficacy. Allosteric modulation heralds a new approach to the manipulation of the endocannabinoid system for therapeutic benefit; it promises to augment the existing portfolio of selective direct agonists, competitive antagonists and enzyme inhibitors.

Original languageEnglish
Pages (from-to)567-572
Number of pages6
JournalTrends in Pharmacological Sciences
Volume28
DOIs
Publication statusPublished - 2007

Keywords

  • protein-coupled receptors
  • endocannabinoid system
  • multiple-sclerosis
  • neutral antagonism
  • inverse agonism
  • bone mass
  • exploitation
  • inflammation
  • ligands
  • pain

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