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三链DNA是一种具有众多生理学功能的生物大分子,可用于基因的表达调控,可以作为一种基因疗法的手段控制基因的转录和调节特定基因的表达。药物小分子与DNA的相互作用对于实现小分子的药理功能并介导相关生理过程都是非常重要的。在过去的几十年里,科学家们付出了很多努力来研究三链核酸的结合剂,然而报道的比较有效的筛选方法并不多。本文从提高TC型三链DNA稳定性的策略、三链DNA与结合剂相互作用的研究方法的原理及应用、研究方法的展望三方面展开论述。主要阐述了平衡透析法、纳米金比色法、多种核酸结构混合变温法、离心超滤法、电喷雾直接进样法、液质联用法和光谱学方法(紫外分光光谱、荧光光谱、圆二色光谱)等几种方法的原理、应用及存在的问题,对小分子配体与三链DNA相互作用的研究具有重要的意义。

Triplex DNA can interfere with gene transcription and expression modulation .It is one kind of important biological macromolecules .The interaction between small molecules and DNA targets plays an important role in the function of drug mediated physiological processes .In the past decades, numerous attempts have been made to screen triplex DNA binders .However, not too many effective methods for screening triplex DNA binders were reported . Basic principles , the screening methods of research and application for the interaction between small ligands and triplex DNA were summarized , including mainly the principle and application of several methods , such as competition dialysis , gold nanoparticle based approach , thermal denaturation method , centrifugal ultrafiltration method , electrospray ionization mass spectroscopy ( MS) method, and liquid chromatography-mass spectroscopy ( LC-MS) combined method .This review has a general instruction to the research of the interaction between small ligands and triplex DNA .

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