Conformational transition of DNA by dinuclear Pt(II) complexes causes cooperative inhibition of gene expression
Conformational transition of DNA by dinuclear Pt(II) complexes causes cooperative inhibition of gene expression
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DOI：
10.1016/j.cplett.2017.04.039
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发表时间：
2017-06-16
影响因子：
2.8
通讯作者：
Yoshikawa, Kenichi
中科院分区：
文献类型：
--
作者：
Shimizu, Yuta;Yoshikawa, Yuko;Yoshikawa, Kenichi
近年来，一种新型的阳离子四唑桥联双核铂（Ⅱ）配合物5-H-Y被报道是一种很有前途的抗肿瘤药物。在这里，我们研究了一系列的四唑桥联双核铂（II）配合物的DNA的高阶结构的影响，通过使用荧光和原子力显微镜。结果表明，双核铂配合物对基因组DNA的构象有明显的收缩作用。我们还发现这些药物对体外基因表达的高度协同抑制作用。从它们对DNA片段的桥接作用方面讨论了这些双核Pt（II）配合物的独特作用机制。(C)2017作者（S）由爱思唯尔公司出版
Recently, it was reported that a cationic tetrazolato-bridged dinuclear Pt(II) complex, 5-H-Y, is a promising anticancer drug candidate. Here, we investigated the effects of a series of tetrazolato-bridged dinuclear Pt(II) complexes on the higher-order structure of DNA by using fluorescence and atomic force microscopies. The results showed that these dinuclear Pt(II) complexes cause marked shrinkage on the conformation of genomic DNA. We also found highly cooperative inhibitory effects of these drugs on in vitro gene expression. The unique mechanism of action of these dinuclear Pt(II) complexes is discussed in terms of their bridging effect on DNA segments. (C) 2017 The Author(s). Published by Elsevier B.V.