Kenakin Terry
Assay Development and Compound Profiling, GlaxoSmithKline Research and Development, Research Triangle Park, NC 27709, USA.
Mol Interv. 2004 Aug;4(4):222-9. doi: 10.1124/mi.4.4.6.
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.
变构拮抗剂可调节激动剂对受体的亲和力和/或效能。尽管这种调节发生的方式可能类似于简单竞争性拮抗剂，但变构拮抗剂具有独特的性质，可能呈现出看似多变的拮抗作用特征。这些独特性质也为治疗应用提供了潜在有用的模式。本综述总结了检测变构拮抗作用的方法以及这些受体调节剂的一些特殊性质。
