DNA topoisomerases catalyze topological changes in DNA that are essential f
or normal cell cycle progression and therefore they are a preferential targ
et for the development of anticancer drugs. Anti-topoisomerase drugs can be
divided into two main classes: "cleavable complex" poisons and catalytic i
nhibitors. The "cleavable complex" poisons are very effective as anticancer
drugs but are also potent inducers of chromosome aberrations so they can c
ause secondary malignancies. Catalytic inhibitors are cytotoxic but they do
not induce chromosome aberrations. Knowledge about the mechanism of action
of topoisomerase inhibitors is important to determine the best anti-topois
omerase combinations, with a reduced risk of induction of secondary maligna
ncies.