Biltonen R L
Fed Proc. 1977 Jul;36(8):2112-4.
Assuming that the biological response is directly proportional to the fractional degree of receptor occupancy, the mathematical relationships between free ligand concentration, receptor occupation and biological activity are developed for a number of equilibrium models. The models considered include simple 1:1 binding with and without conformational changes in the receptor, the coupled binding of two distinct effectors to a single macromolecule, and a system involving indirect coupling between two effectors that bind to two distinct components of the receptor system. This latter model is elaborated into the concept of a domain of receptor-enzyme pairs such that occupation of a single receptor may activate the entire domain of enzymes. This model can explain discrepancies between activation and binding isotherms as has been found with some beta-adrenergic agonist-sensitive adenylate cyclase systems.
假设生物反应与受体占据的分数程度成正比，针对多种平衡模型建立了游离配体浓度、受体占据和生物活性之间的数学关系。所考虑的模型包括受体存在和不存在构象变化时的简单1:1结合、两种不同效应物与单个大分子的偶联结合，以及涉及两种效应物之间间接偶联的系统，这两种效应物分别与受体系统的两个不同组分结合。后一种模型被细化为受体 - 酶对结构域的概念，使得单个受体的占据可激活整个酶结构域。该模型可以解释一些β - 肾上腺素能激动剂敏感的腺苷酸环化酶系统中发现的激活等温线和结合等温线之间的差异。
