拓扑异构酶和蒽环类药物：在抗癌治疗和心脏毒性预防过程中的研究进展和展望

Title:Topoisomerases and Anthracyclines: Recent Advances and Perspectives in Anticancer Therapy and Prevention of Cardiotoxicity

Volume: 24 Issue: 15

关键词: 蒽环类药物，肿瘤化疗，心脏肿瘤，心脏毒性，催化抑制剂，DNA拓扑异构酶，拓扑异构酶抑制剂。

摘要: Topoisomerases are ubiquitous enzymes involved in maintaining genomic stability of the cell by regulating the over- or underwinding of DNA strands. Besides their customary functions, topoisomerases are important cellular targets of widely used anticancer drugs. In particular, topoisomerase IIα (Top2α) has been postulated as the primary molecular target of anthracycline’s anticancer activity, whereas topoisomerase IIβ (Top2β), the only Top2 present in heart tissue, seems to be involved in the development of anthracycline-induced cardiotoxicity. Noteworthy, cardiotoxicity is the most frequent adverse effect of both conventional and modern anticancer targeted therapy, representing the leading noncancer-related cause of morbidity and mortality in long-term survivors. The molecular mechanisms of anthracyclineinduced cardiotoxicity have been investigated for decades and, despite the numerous mechanistic hypotheses put forward, its aetiology and pathogenesis still remain controversial.

Cite this article as:

Topoisomerases and Anthracyclines: Recent Advances and Perspectives in Anticancer Therapy and Prevention of Cardiotoxicity, Current Medicinal Chemistry 2017; 24 (15) . https://dx.doi.org/10.2174/0929867323666161214120355