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[DNA拓扑异构酶抑制剂]

[Inhibitors of DNA topoisomerases].

作者信息

Andoh T

机构信息

Dept. of Bioengineering, Soka University Faculty of Engineering.

出版信息

Gan To Kagaku Ryoho. 1997 Sep;24(11):1526-35.

PMID:9309151
Abstract

DNA topoisomerases are enzymes regulating the conformational state of DNA in every aspect of genetic processes by catalyzing transient cleavage and religation of DNA strands. The enzymes are targets of some of the important anticancer drugs. Many candidates of anticancer drugs are being screened via inhibition of the enzymes. In the present review, I discuss the role of DNA topoisomerases in genetic processes in mammalian cells, characteristics and mode of action of topoisomerase inhibitors, and resistance of tumor cells to the anticancer drugs.

摘要

DNA拓扑异构酶是一类通过催化DNA链的瞬时切割和重新连接来调节遗传过程各个方面中DNA构象状态的酶。这些酶是一些重要抗癌药物的作用靶点。许多抗癌药物候选物正在通过抑制这些酶进行筛选。在本综述中,我将讨论DNA拓扑异构酶在哺乳动物细胞遗传过程中的作用、拓扑异构酶抑制剂的特性和作用方式,以及肿瘤细胞对抗癌药物的耐药性。

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