靶向拓扑异构酶I的药物喜树碱类似物的最新进展。

Recent advances in topoisomerase I-targeting agents, camptothecin analogues.

作者信息

Kim Dae-Kee, Lee Namkyu

机构信息

Life Science Research Center, SK Chemicals, 600 Jungja-Dong, Changan-Ku, Suwon-Si, Kyungki-Do 440-745, Korea.

出版信息

Mini Rev Med Chem. 2002 Dec;2(6):611-9. doi: 10.2174/1389557023405530.

DOI:10.2174/1389557023405530

PMID:12370044

Abstract

The present review concentrates on camptothecin (CPT) analogues, the most extensively studied topoisomerase I (topo I) inhibitors, and provides concise information on the structural features of human topo I enzyme, mechanisms of interaction of CPT with topo I, structure-activity relationship study of CPT analogues including the influence of lactone stability on antitumor activity, and recent updates of valuable CPT analogues.

摘要

本综述聚焦于喜树碱（CPT）类似物，这是研究最为广泛的拓扑异构酶I（topo I）抑制剂，并提供了关于人类topo I酶结构特征、CPT与topo I相互作用机制、CPT类似物构效关系研究（包括内酯稳定性对抗肿瘤活性的影响）以及有价值的CPT类似物的最新进展等方面的简要信息。