Leff P
Department of Pharmacology, Fisons, Loughborough, UK.
Trends Pharmacol Sci. 1995 Mar;16(3):89-97. doi: 10.1016/s0165-6147(00)88989-0.
Over the past few years, the concept that the activation of G protein-coupled receptors and transmitter-gated ion channels depends on a conformational change has received increasingly widespread acceptance. As a result, these two structurally distinct families of receptors can now be considered to obey a similar two-state mechanism. However, traditional receptor theory has largely overlooked this concept. In this article, Paul Leff explains and illustrates the predictions of the two-state model of receptor activation and discusses its impact on the analysis and interpretation of agonist-receptor interactions.
在过去几年中，G蛋白偶联受体和递质门控离子通道的激活依赖于构象变化这一概念已得到越来越广泛的认可。因此，现在可以认为这两个结构不同的受体家族遵循类似的双态机制。然而，传统的受体理论在很大程度上忽略了这一概念。在本文中，保罗·莱夫解释并阐述了受体激活双态模型的预测，并讨论了其对激动剂-受体相互作用分析和解释的影响。
