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首页> 外文期刊>Biochemistry >INTERACTION OF A DNA-THREADING NETROPSIN-AMSACRINE COMBILEXIN WITH DNA AND CHROMATIN
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INTERACTION OF A DNA-THREADING NETROPSIN-AMSACRINE COMBILEXIN WITH DNA AND CHROMATIN

机译：脱氧核糖核酸神经肽-氨苄青霉素复合物与DNA和染色质的相互作用

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摘要

Combilexins are a group of DNA ligands having a sequence-specific minor groove binding element combined with an intercalating chromophore which stabilizes the DNA complex and can interfere with topoisomerases. In this study, complementary methods of spectroscopy (absorption, circular dichroism, electric linear dichroism) and biochemistry (viscometry, footprinting) have been applied to explore the nature of the complex formed between a new amsacrine-4-carboxamide-netropsin combilexin and DNA or chromatin. Collectively, the structural and kinetic data concur that the conjugate threads through the DNA double helix so as to intercalate its acridine chromophore, leaving the netropsin moiety and the methanesulfonanilino group positioned within the minor and major grooves of the double helix, respectively. The hybrid retains the AT selectivity conferred by the netropsin moiety. The threading-type intercalation process, evidenced by stopped-flow measurements, is affected when the DNA is wrapped around histones. The composite drug can bind to both the DNA linker segments and the nucleosomal cores in chromatin though, unlike its constituents, it antagonizes the salt-induced condensation of chromatin. As far as its mode of binding to DNA is concerned, the netropsin-amsacrine hybrid molecule exhibits structural features reminiscent of the antitumor antibiotics nogalamycin and pluramycin. The design of DNA-threading combilexins provides an original route for the development of sequence-specific ligands capable of forming stable complexes with DNA.
机译：Combilexins是一组DNA配体，具有序列特异性小沟结合元件和嵌入发色团，该发色团稳定了DNA复合物并可以干扰拓扑异构酶。在这项研究中，已应用光谱学（吸收，圆二色性，线性线性二色性）和生物化学（粘度测定，足迹法）的互补方法来探索新的amsacrine-4-carboxamide-netropsin combilexin和DNA之间形成的复合物的性质。染色质。总的来说，结构和动力学数据认为，缀合物穿过DNA双螺旋，从而插入其a啶发色团，从而使netropsin部分和甲磺酰苯胺基分别位于双螺旋的小和大凹槽内。杂种保留了由netropsin部分赋予的AT选择性。当DNA包裹在组蛋白周围时，通过停流测量证明的穿线型插入过程会受到影响。该复合药物可与染色质中的DNA接头片段和核小体核心结合，尽管与它的成分不同，它可拮抗盐诱导的染色质缩合。就其与DNA的结合方式而言，netropsin-amsacrine杂合分子的结构特征让人联想到抗肿瘤抗生素Nogalamycin和pluramycin。 DNA穿刺梳理蛋白的设计为开发能够与DNA形成稳定复合物的序列特异性配体提供了一条原始途径。

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