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首页> 外文期刊>Chemistry: A European journal >Chemo-genetic optimization of DNA recognition by metallodrugs using a presenter-protein strategy
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Chemo-genetic optimization of DNA recognition by metallodrugs using a presenter-protein strategy

机译：使用呈递蛋白策略对金属药物进行DNA识别的化学遗传优化

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摘要

The mode of action of precious metal anticancer metallodrugs is generally believed to involve DNA as a target. However, the poor specificity of such drugs often requires high doses and leads to undesirable side-effects. With the aim of improving the specificity of a ruthenium piano-stool complex towards DNA, we employed a presenter protein strategy based on the biotinavidin technology. Guided by the X-ray structure of the assembly of streptavidin and a biotinylated piano-stool, we explored the formation of metallodrug-mediated ternary complexes with the presenter protein and DNA. The assemblies bound more strongly to telomere G-quadruplexes than to double-stranded DNA; chemo-genetic modifications (varying the complex or mutating the protein) modulated binding to these targets. We suggest that rational targeting of small molecules by presenter proteins could be exploited to bind metallodrugs to preferred macromolecular targets.
机译：通常认为贵金属抗癌金属药物的作用方式涉及DNA作为靶标。但是，这类药物的特异性差通常需要高剂量，并导致不良的副作用。为了提高钌钢琴凳复合物对DNA的特异性，我们采用了基于biotinavidin技术的呈递蛋白策略。在链霉亲和素和生物素化的钢琴凳的装配体的X射线结构指导下，我们探索了呈递蛋白和DNA的金属药物介导的三元复合物的形成。装配体与端粒G-四链体的结合比与双链DNA的结合更牢固。化学遗传修饰（改变复合物或突变蛋白质）可调节与这些靶标的结合。我们建议可以利用呈递蛋白对小分子进行合理靶向，从而将金属药物与优选的大分子靶标结合。

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