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海洋抗癌药物中变体林 B 的嵌入性 DNA 结合。

Intercalative DNA binding of the marine anticancer drug variolin B.

机构信息

Institute for Research in Biomedicine (IRB Barcelona), The Barcelona Institute of Science and Technology, Baldiri Reixac 10, 08028 Barcelona, Spain.

Institut de Biologia Molecular de Barcelona (CSIC), Barcelona Science Park, Baldiri Reixac 10, 08028 Barcelona, Spain.

出版信息

Sci Rep. 2017 Jan 4;7:39680. doi: 10.1038/srep39680.

Abstract

Variolin B is a rare marine alkaloid that showed promising anti-cancer activity soon after its isolation. It acts as a cyclin-dependent kinase inhibitor, although the precise mechanism through which it exerts the cytotoxic effects is still unknown. The crystal structure of a variolin B bound to a DNA forming a pseudo-Holliday junction shows that this compound can also contribute, through intercalative binding, to either the formation or stabilization of multi-stranded DNA forms.

摘要

变洛林 B 是一种罕见的海洋生物碱,在分离后不久就显示出有希望的抗癌活性。它作为一种细胞周期蛋白依赖性激酶抑制剂发挥作用,尽管其发挥细胞毒性作用的确切机制尚不清楚。变洛林 B 与形成假 Holliday 结的 DNA 结合的晶体结构表明,该化合物还可以通过嵌入结合促进多链 DNA 形成或稳定。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/eee0/5209663/81da14062ddd/srep39680-f1.jpg

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