DNA拓扑异构酶Ⅱ抑制剂研究进展

Development of DNA Topoisomerase Ⅱ inhibitors

在DNA复制,转录和有丝分裂等重要的生命过程中,拓扑异构酶Ⅱ是一种重要的酶。拓扑异构酶Ⅱ抑制剂是一种重要的药物,用于包括乳腺癌,肺癌,睾丸癌,淋巴瘤和肉瘤在内的多种恶性肿瘤的治疗。本文综述了几种拓扑异构酶Ⅱ抑制剂的作用机制,毒性,药理和临床应用,这些抑制剂包括依托泊苷,替尼泊苷,多柔比星,柔红霉素,表柔比星,伊达比星和米托蒽醌。本文将着重讲述关于这些药物以及拓扑异构酶Ⅱ抑制剂的发展情况的新信息。

Topoisomerase Ⅱ is an enzyme, important for DNA replication, transcription, mitosis and other vital process. Inhibitors of topoisomerase Ⅱ are important drugs used in the therapy of many neoplasms including breast cancer, lung cancer, testicular cancer, lymphomas and sarcomas. This paper reviews the mechanism of action, toxicities, pharmacology and clinical use of topoisomerase Ⅱ inhibitors including etoposide, teniposide, doxorubicin, daunorubicin, epirubicin, idarubicin and mitoxantrone. New information regarding these agents and those under development is highlighted.