title: A carboline derivative as a novel mammalian DNA topoisomerase II targeting agent.
abstract: 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.
authors.affiliation: Laboratoire de Biochimie-Enzymologie, URA 158 du CNRS, U 140 de l'INSERM, Institut Gustave Roussy, Villejuif, France.
authors.forename: F
authors.initials: F
authors.lastname: Pognan
authors.forename: J M
authors.initials: JM
authors.lastname: Saucier
authors.forename: C
authors.initials: C
authors.lastname: Paoletti
authors.forename: L
authors.initials: L
authors.lastname: Kaczmarek
authors.forename: P
authors.initials: P
authors.lastname: Nantka-Namirski
authors.forename: M
authors.initials: M
authors.lastname: Mordarski
authors.forename: W
authors.initials: W
authors.lastname: Peczynska-Czoch
mesh_terms: D000677:Amsacrine / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000633:toxicity; D002243:Carbolines / Q000494:pharmacology* / Q000633:toxicity; D002417:Cattle; D002478:Cells, Cultured; D006224:Cricetinae; D003412:Cricetulus; D004247:DNA / Q000187:drug effects* / Q000378:metabolism; D004250:DNA Topoisomerases, Type II / Q000187:drug effects* / Q000378:metabolism; D004355:Drug Stability; D007364:Intercalating Agents / Q000494:pharmacology / Q000633:toxicity; D027383:Papillomaviridae / Q000235:genetics; D051381:Rats
chemical_list: D000970:Antineoplastic Agents; D002243:Carbolines; D007364:Intercalating Agents; D000677:Amsacrine; C055575:5,11-dimethyl-5H-indolo(2,3-b)quinoline; D004247:DNA; D004250:DNA Topoisomerases, Type II