Allosteric modulators: the new generation of receptor antagonist.
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.
Kenakin
Terry
T
Assay Development and Compound Profiling, GlaxoSmithKline Research and Development, Research Triangle Park, NC 27709, USA. Terry.P.Kenakin@gsk.com
D000494:Allosteric Regulation; D006801:Humans; D011485:Protein Binding; D011956:Receptors, Cell Surface / Q000037:antagonists & inhibitors* / Q000378:metabolism
D011956:Receptors, Cell Surface