拓扑异构酶Ⅰ天然产物抑制剂的研究进展

Progress on natural products as inhibitors of topoisomeraseⅠ

DNA拓扑异构酶Ⅰ(topoisomeraseⅠ,TopoⅠ)参与DNA的复制、转录、重组和修复等所有关键的核过程。近几年,其抗肿瘤小分子抑制剂的研究逐渐成为热点。该文对21世纪以来报道的新拓扑异构酶Ⅰ天然产物抑制剂的结构、生物活性及结构改造等进行系统的综述,以期为设计全新结构的拓扑异构酶Ⅰ抑制剂提供指导。

Topoisomerases Ⅰ（Topo Ⅰ） are nuclear enzymes that catalyze the concerted breaking and rejoining of DNA strands such as replication,recombination,and transcription.In recent years,research on small molecule TopoⅠ inhibitors has gradually become a hot spot.Systematically the progress in structures,biological activity,and structural modification of the natural products as Topo Ⅰ inhibitors since 2000 were reviewed.It is expected that this review will provide a guidance to the rational design of Topo Ⅰ inhibitors.