拓扑异构酶Ⅰ和Ⅱ双重抑制剂的研究进展

蒋琰; 盛春泉; 董国强

doi:10.3969/j.issn.1006-0111.2015.04.004

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拓扑异构酶Ⅰ和Ⅱ双重抑制剂的研究进展

蒋琰, 盛春泉, 董国强

文章导航 > 药学实践与服务 > 2015 > 33(4): 303-308,379

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]. 药学实践与服务, 2015, 33(4): 303-308,379. doi: 10.3969/j.issn.1006-0111.2015.04.004

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]. 药学实践与服务, 2015, 33(4): 303-308,379. doi: 10.3969/j.issn.1006-0111.2015.04.004

JIANG Yan, SHENG Chunquan, DONG Guoqiang. Research progress of dual topoisomerase Ⅰ and Ⅱ inhibitors[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 303-308,379. doi: 10.3969/j.issn.1006-0111.2015.04.004

Citation:

JIANG Yan, SHENG Chunquan, DONG Guoqiang. Research progress of dual topoisomerase Ⅰ and Ⅱ inhibitors[J]. Journal of Pharmaceutical Practice and Service, 2015, 33(4): 303-308,379. doi: 10.3969/j.issn.1006-0111.2015.04.004

拓扑异构酶Ⅰ和Ⅱ双重抑制剂的研究进展

doi: 10.3969/j.issn.1006-0111.2015.04.004

第二军医大学药学院药物化学教研室, 上海 200433

Research progress of dual topoisomerase Ⅰ and Ⅱ inhibitors

Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

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。
- TopⅠ /
- TopⅡ /
- 双重抑制剂 /
- 抗肿瘤药物
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.
- topoisomerase Ⅰ /
- topoisomerase Ⅱ /
- dual inhibitors /
- anticancer drugs

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拓扑异构酶Ⅰ和Ⅱ双重抑制剂的研究进展

doi: 10.3969/j.issn.1006-0111.2015.04.004

第二军医大学药学院药物化学教研室, 上海 200433

收稿日期: 2013-10-15
修回日期: 2014-02-19

关键词:

TopⅠ /

TopⅡ /

双重抑制剂 /

抗肿瘤药物

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。