Screening of DNA topoisomerase inhibitors

摘要

It has been established that etoposide (ETP), adriamycin (doxorubicin: DOX) and irinotecan (CPT-11), efficacious antitumor drugs widely used in clinics, target DNA topoisomerases (topo) in vivo. The present report attempts to explain why topos are the good targets of anticancer drugs from the point of view of enzymology of the enzymes and cell cycle behavior of tumor cells. Thus, many candidate anticancer drugs targeting topos are being screened, and preclinical and clinical studies thereof are being conducted world-wide and in Japan.