The two-state model of receptor activation.
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.
Leff
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Department of Pharmacology, Fisons, Loughborough, UK.
D001667:Binding, Competitive; D015195:Drug Design; D019204:GTP-Binding Proteins / Q000378:metabolism*; D007473:Ion Channels / Q000378:metabolism* / Q000502:physiology; D008024:Ligands; D008956:Models, Chemical; D011956:Receptors, Cell Surface / Q000819:agonists / Q000378:metabolism*
D007473:Ion Channels; D008024:Ligands; D011956:Receptors, Cell Surface; D019204:GTP-Binding Proteins