大学化学 >> 2014, Vol. 29 >> Issue (1): 1-10.doi: 10.3969/j.issn.1000-8438.2014.01.001

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靶向抑制DNA拓扑异构酶的抗肿瘤药物研究

钱晨, 彭再利, 巢晖   

  1. 中山大学化学与化学工程学院 广东广州 510275
  • 发布日期:2014-02-25

Targeting Inhibition of DNA Topoisomerases by Antitumor Drugs

Qian Chen, Peng Zaili, Chao Hui   

  1. School of Chemistry and Chemical Engineering, Sun Yat-sen University, Guangzhou 510275, Guangdong Province, P. R. China
  • Published:2014-02-25

摘要: DNA拓扑异构酶是真核细胞和原核细胞中的一种基本酶,广泛存在于细胞核中,对DNA的转录、复制以及基因表达过程中的DNA拓扑结构的改变起着重要的作用。研究发现DNA拓扑异构酶在肿瘤组织中高度表达,许多抗肿瘤药物的作用机制与抑制拓扑异构酶有关,目前拓扑异构酶已成为筛选抗肿瘤药物的重要靶点。

关键词: DNA拓扑异构酶, 抑制剂, 抗肿瘤药物

Abstract: DNA topoisomerases are ubiquitous enzymes in eukaryotic cell and prokaryotic cell. They are widely existing in the nucleus and playing a crucial role in cellular genetic processing, such as transcription,replication and gene expression. Recent studies show that, topoisomerases are over expressed in cancer cell and thus they have become the important targets for screening of antitumor drug.

Key words: DNA topoisomerase, DNA topoisomerase inhibitor, anticancer drug