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Biochem Pharmacol. 1992 Dec 1;44(11):2149-55.

A carboline derivative as a novel mammalian DNA topoisomerase II targeting agent.

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  • 1Laboratoire de Biochimie-Enzymologie, URA 158 du CNRS, U 140 de l'INSERM, Institut Gustave Roussy, Villejuif, France.


The DNA intercalating, ellipticine analog drug, 5,11-dimethyl-5H-indol[2,3-b]quinoline, is able to stabilize in vitro the topoisomerase II-DNA cleavable complex and to induce DNA breaks in BPV I episome in rat fibroblasts. Cytotoxicity studies with DC3F cells resistant to ellipticine strongly suggest that topoisomerase II is a cellular target involved in the mechanism of cytotoxic action of this carboline derivative.

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