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 language | English |
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Pages (from-to) | 567-572 |
Number of pages | 6 |
Journal | Trends in Pharmacological Sciences |
Volume | 28 |
DOIs | |
Publication status | Published - 2007 |
Keywords
- protein-coupled receptors
- endocannabinoid system
- multiple-sclerosis
- neutral antagonism
- inverse agonism
- bone mass
- exploitation
- inflammation
- ligands
- pain