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Molecular Interventions 4:222-229, (2004)
© American Society for Pharmacology and Experimental Therapeutics
10.1124/mi.4.4.6
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Review

Allosteric Modulators: The New Generation of Receptor Antagonist

Terry Kenakin

Assay Development and Compound Profiling, GlaxoSmithKline Research and Development, Research Triangle Park, NC 27709


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.




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