药物-受体-DNA 系统中竞争结合的一般分析。

General analysis of competitive binding in drug-interceptor-DNA systems.

机构信息

Department of Physics, Sevastopol National Technical University, Universitetskaya str., 33, Sevastopol 99053, Ukraine.

出版信息

Eur Biophys J. 2012 Mar;41(3):273-83. doi: 10.1007/s00249-011-0783-3. Epub 2012 Jan 3.

Abstract

A general model of competitive binding in drug-interceptor-DNA systems has been developed in order to quantify both the interceptor and protector mechanisms. The model involves full parameterization of the basic equations governing the mutual competition between drugs binding to DNA and incorporates as partial cases various similar models existing in the literature. The generality of the model results from strict accounting of the statistical effects of the binding of the drug and interceptor with DNA according to the McGhee-von Hippel formalism, and to the strict treatment of hetero-association between the drug and interceptor, which includes formation of all possible types of self- and hetero-complexes in solution. Indirect experimental evidence is provided for the importance of the protector mechanism in drug-caffeine-DNA systems, which is sometimes ignored in the literature because of the small magnitude of the CAF-DNA binding constant.

摘要

为了定量描述受体和保护剂的作用机制,建立了药物-受体-DNA 系统的竞争结合的一般模型。该模型对控制药物与 DNA 相互竞争的基本方程进行了全面参数化,并将文献中存在的各种类似模型作为特例纳入其中。该模型的通用性源于根据 McGhee-von Hippel 形式主义严格核算药物和受体与 DNA 结合的统计效应,以及对药物和受体之间的异源缔合的严格处理,其中包括在溶液中形成所有可能类型的自和异源复合物。为了说明保护剂机制在药物-咖啡因-DNA 系统中的重要性,提供了间接的实验证据,而在文献中,由于 CAF-DNA 结合常数的幅度较小,该机制有时会被忽略。

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