title: Allosterism and cannabinoid CB(1) receptors: the shape of things to come.
abstract: In 2005, the first evidence was obtained that the cannabinoid CB(1) 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.
authors.affiliation: Institute of Medical Sciences, University of Aberdeen, Aberdeen, AB25 2ZD, UK. r.ross@abdn.ac.uk
authors.forename: Ruth A
authors.initials: RA
authors.lastname: Ross
mesh_terms: D000494:Allosteric Regulation / Q000187:drug effects; D000818:Animals; D006801:Humans; D008024:Ligands; D008954:Models, Biological; D015394:Molecular Structure; D043884:Receptor, Cannabinoid, CB1 / Q000819:agonists* / Q000037:antagonists & inhibitors
chemical_list: D008024:Ligands; D043884:Receptor, Cannabinoid, CB1