Tuk B, van Oostenbruggen M F
Division of Pharmacology, Leiden/Amsterdam Center for Drug Research, Leiden University, The Netherlands.
Trends Pharmacol Sci. 1996 Nov;17(11):403-9. doi: 10.1016/s0165-6147(96)10049-3.
According to the occupation model, the observed sigmoidicity in receptor-binding studies frequently yields non-integer values for the number of molecules that bind per receptor, which may suggest inconsistencies of the model. Here, Bertil Tuk and Michael van Oostenbruggen re-examine the derivation of the model and pinpoint the origin of the observed inconsistencies, thereby demonstrating that these inconsistencies may lead to substantial error in estimates of receptor affinity, number of molecules that bind per receptor and cooperativity. A reformulated model allows more information to be derived from receptor-binding experiments, yielding integer estimates of the number of molecules that bind per receptor and quantitatively estimating the degree of cooperativity.
根据占据模型,在受体结合研究中观察到的S形曲线常常导致每个受体结合的分子数出现非整数值,这可能暗示该模型存在不一致性。在此,伯蒂尔·图克和迈克尔·范·奥斯坦布鲁根重新审视了该模型的推导过程,并指出了观察到的不一致性的根源,从而证明这些不一致性可能会在受体亲和力、每个受体结合的分子数以及协同性的估计中导致重大误差。一个重新制定的模型能够从受体结合实验中获取更多信息,得出每个受体结合的分子数的整数值,并定量估计协同程度。