Binding, gating, affinity and efficacy: The interpretation of structure-activity relationships for agonists and of the effects of mutating receptors

Abstract

It seems that there is still insufficient knowledge of mechanisms of G protein-coupled receptors to allow the unambiguous inferences about whether receptor mutations affect the primary binding reaction or later conformation changes. Therefore many inferences about the nature of the agonist-binding site lack any rational basis. Until we have detailed structures, we shall not know how many of them are wrong. It will be very interesting to find out.