title: Inhibition of human topoisomerases I and II by simocyclinone D8.
abstract: Simocyclinone D8 is an antibiotic isolated from Streptomyces antibioticus Tü 6040 that inhibits the supercoiling activity of DNA gyrase. It also exhibits an inhibitory effect on human topoisomerase II and an antiproliferative activity against some cancer cell lines. Our biochemical studies have revealed that simocyclinone D8 can inhibit the catalytic activity of human topoisomerase I. Thus, simocyclinone D8 is a dual catalytic inhibitor of human topoisomerases I and II.
authors.affiliation: Department of Pharmacology, University of Minnesota Medical School, Minneapolis, MN 55455, USA.
authors.forename: Lisa M
authors.initials: LM
authors.lastname: Oppegard
authors.forename: Thuy
authors.initials: T
authors.lastname: Nguyen
authors.forename: Keith C
authors.initials: KC
authors.lastname: Ellis
authors.forename: Hiroshi
authors.initials: H
authors.lastname: Hiasa
mesh_terms: D003374:Coumarins / Q000737:chemistry / Q000494:pharmacology; D004264:DNA Topoisomerases, Type I / Q000378:metabolism; D004250:DNA Topoisomerases, Type II / Q000378:metabolism; D006027:Glycosides / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D015394:Molecular Structure; D013303:Streptomyces antibioticus; D059004:Topoisomerase I Inhibitors / Q000494:pharmacology*; D059005:Topoisomerase II Inhibitors / Q000494:pharmacology*
chemical_list: D003374:Coumarins; D006027:Glycosides; D059004:Topoisomerase I Inhibitors; D059005:Topoisomerase II Inhibitors; C416814:simocyclinone D8; D004264:DNA Topoisomerases, Type I; D004250:DNA Topoisomerases, Type II