Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, NC 27599- 7365, USA.
Curr Top Med Chem. 2013;13(1):5-13. doi: 10.2174/1568026611313010003.
Seven transmembrane Receptors (7TMRs) transmit signals through changes in conformation; the binding of ligands to any site on the receptor has the potential to change the receptor conformation. Allosteric ligands are defined as those which bind to sites other than the one needed for the endogenous receptor agonist (neurotransmitters, hormones). Allosteric ligand function is saturable (comes to a finite magnitude when the allosteric site is fully occupied) and probe dependent (the effects vary with different co-binding ligands). Both direct effects on receptor conformation and the induced effect on endogenous ligands must be considered when describing allosteric ligands; this paper will describe the quantitative models available to characterize these allosteric effects in molecular terms which can then be used to predict allosteric effects in all systems.
七跨膜受体（7TMRs）通过构象变化传递信号；配体与受体上任何部位的结合都有可能改变受体构象。变构配体的定义是那些与内源性受体激动剂（神经递质、激素）所需结合部位不同的配体。变构配体的功能是饱和的（当变构部位完全占据时，达到有限的幅度），并且依赖于探针（不同的共同结合配体的作用不同）。在描述变构配体时，必须考虑对受体构象的直接影响以及对内源性配体的诱导效应；本文将描述可用的定量模型，以从分子角度描述这些变构效应，然后可以用于预测所有系统中的变构效应。
