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

Alvaro Mordente, Elisabetta Meucci, Daniela Tavian, Andrea Silvestrini, Giuseppe Ettore Martorana

Research output: Contribution to journalArticlepeer-review

22 Citations (Scopus)


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 II β (Top2β), the only Top2 present in heart tissue, seems to be involved into 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 anthracycline-induced cardiotoxicity have been investigated for decades and, despite the numerous mechanistic hypotheses put forward, its aetiology and pathogenesis still remain controversial. This review is aimed at focusing on the double edge sword of topoisomerase-anthracycline interaction, and, in particular, on the potential role of topoisomerases in anthracyclines anticancer activity as well as in the pathogenesis of anthracycline-induced cardiotoxicity.
Original languageEnglish
Pages (from-to)1-24
Number of pages24
Publication statusPublished - 2016


  • topoisomerases


Dive into the research topics of 'Topoisomerases and Anthracyclines: Recent Advances and Perspectives in Anticancer Therapy and Prevention of Cardiotoxicity'. Together they form a unique fingerprint.

Cite this