Can DNA intercalators function as topoisomerase inhibitors?
The DNA unwinding suggests DNA intercalation, which could explain the inhibition of topoisomerase II. Among its many properties, amiloride is a DNA intercalator and topoisomerase II inhibitor. Amsacrine, a DNA intercalator and topoisomerase II inhibitor, is efficacious as an antileukemogenic agent. AQ4N (1,4-bis[[2-(dimethylamino)ethyl] amino]-5,8-dihydroxyanthracene-9, 10-dione bis-N-oxide dihydrochloride) is a prodrug which is selectively activated within hypoxic tissues to AQ4, a topoisomerase II inhibitor and DNA intercalator. Amonafide is a DNA intercalator and topoisomerase II inhibitor in clinical development for the treatment of neoplastic diseases.