| 拓扑异构酶Ⅰ和Ⅱ双重抑制剂的研究进展 |
| 投稿时间：2013-10-15 修订日期：2014-02-19 点此下载全文 |
| 引用本文：蒋琰,盛春泉,董国强.拓扑异构酶Ⅰ和Ⅱ双重抑制剂的研究进展[J].药学实践杂志,2015,33(4):303~308,379 |
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| 中文摘要:拓扑异构酶(topoisomerases,Tops)是参与调节细胞内DNA复制、转录、重组和修复等过程的必需酶。Tops分为TopⅠ和TopⅡ,两者通过DNA切断和连接,维持DNA正常拓扑结构和代谢过程。由于Tops在DNA代谢过程的重要作用,干扰Tops的催化活性或者诱导产生Tops介导的DNA损伤已经成为抗肿瘤治疗的重要策略。Tops已经成为最重要的抗肿瘤靶点之一。综述近年来Tops双重抑制剂的研究进展。 |
| 中文关键词:TopⅠ TopⅡ 双重抑制剂 抗肿瘤药物 |
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| Research progress of dual topoisomerase Ⅰ and Ⅱ inhibitors |
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| Abstract:DNA topoisomerases (Tops) are essential enzymes that regulate the cellular processes such as replication, transcription, recombination and repair. DNA Tops can be classified into two types, topoisomerase Ⅰ (TopⅠ) and topoisomerase Ⅱ (TopⅡ). They catalyze the breakage and religation of DNA, maintaining the topological changes of DNA and various DNA metabolic processes. Due to their important role in DNA metabolism, the ability to interfere with the functions of Tops or generating Top-mediated DNA damage is an effective strategy for cancer chemotherapy. Tops have been considered as the most important targets for tumor chemotherapy. In this review, we used examples to describe the development of dual topoisomerase Ⅰ and Ⅱ inhibitors. |
| keywords:topoisomerase Ⅰ topoisomerase Ⅱ dual inhibitors anticancer drugs |
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