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特定类固醇-蛋白质结合的竞争性抑制:相对竞争比在推导平衡抑制常数中的实际应用。

Competitive inhibition of specific steroid-protein binding: practical use of relative competition ratios for the derivation of equilibrium inhibition constants.

作者信息

Blondeau J P, Rocher P, Robel P

出版信息

Steroids. 1978 Dec;32(5):563-75. doi: 10.1016/0039-128x(78)90068-5.

DOI:10.1016/0039-128x(78)90068-5
PMID:734692
Abstract

The relative competition ratio (RCR) is widely used to express the relative affinities of inhibitor(s) and agonist for a binding protein. The RCR is not a constant; it depends on the concentrations of binding sites and of radioactive hormone, and on the presence of nonsaturable binding component(s). According to the assay conditions used, equating the RCR value to the ratio Ka/Ki of the equilibrium association constants of agonist and inhibitor can lead to large errors. In the case of homogeneous non-interacting binding sites, simple correction factors permit one to calculate the ratio Ka/Ki from the measured RCR value. Calculations are given for the eventual contribution of nonsaturable binding components. Corrections can be unnecessary under well defined experimental conditions, where the bound fraction of hormone in absence of competitor is reduced by using a large dilution of binding protein and/or an increased concentration of radioactive hormone.

摘要

相对竞争率(RCR)被广泛用于表示抑制剂和激动剂与结合蛋白的相对亲和力。RCR不是一个常数;它取决于结合位点和放射性激素的浓度,以及非饱和结合成分的存在。根据所使用的测定条件,将RCR值等同于激动剂和抑制剂的平衡缔合常数的Ka/Ki比值可能会导致很大的误差。在均匀非相互作用结合位点的情况下,简单的校正因子允许人们从测量的RCR值计算Ka/Ki比值。给出了非饱和结合成分最终贡献的计算方法。在明确的实验条件下,校正可能是不必要的,即在不存在竞争者的情况下,通过大量稀释结合蛋白和/或增加放射性激素的浓度来降低激素的结合分数。

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