摘要
拓扑异构酶Ⅰ(topoisomerase,Topo)参与DNA复制、转录、重组、修复等所有关键的细胞核内过程,是抗肿瘤研究的重要靶点,以TopoⅠ为靶点的药物在肿瘤化疗中被广泛应用。目前临床使用或处于临床前研究的拓扑异构酶Ⅰ抑制剂主要分为喜树碱类和非喜树碱类化合物。该文主要介绍了近年来TopoⅠ抑制剂研发领域的最新进展和发展趋势,并就近年来涌现出的一些新的TopoⅠ抑制剂的抗肿瘤活性和药理学特性做一总结。
Following the realization that involved in all of the key process within the cell nucleus such as DNA replication, transcription, reorganization, repair, human DNA topoisomerase Ⅰ （Topo Ⅰ ） is a useful therapeutic target against tumor growth. Topo Ⅰ inhibitors represent a class of effective agents that have been extensively exploited and used for carcinomachemotherapy. Current Topo Ⅰ inhibitors being clinically used or developed are classified as campotothecins and non-camptothecins. This presentation introduces current status and trends of Topo Ⅰ inhibitots as anti-tumor agents with an emphasis on bioactive and pharmacological properties of these agents.
出处
《中国药理学通报》
CAS
CSCD
北大核心
2009年第4期436-441,共6页
Chinese Pharmacological Bulletin
