title: CJ-12,373, a novel topoisomerase II inhibitor: fermentation, isolation, structure elucidation and biological activities.
abstract: A novel isochroman carboxylic acid CJ-12,373 was isolated from Penicillium sp. CL22557. CJ-12,373 inhibits both DNA gyrase-mediated supercoiling and relaxation without the formation of a cleavage intermediate, suggesting that CJ-12,373 inhibits DNA gyrase at a stage distinct from the religation step. CJ-12,373 is not selective for procaryotic DNA gyrase as it also inhibits relaxation mediated by eukaryotic topoisomerase II. The antimicrobial potency of CJ-12,373, however, is largely attributed to its inhibition of DNA gyrase.
authors.affiliation: Central Research Division, Pfizer Pharmaceuticals Inc., Aichi, Japan.
authors.forename: T
authors.initials: T
authors.lastname: Inagaki
authors.forename: K
authors.initials: K
authors.lastname: Kaneda
authors.forename: Y
authors.initials: Y
authors.lastname: Suzuki
authors.forename: H
authors.initials: H
authors.lastname: Hirai
authors.forename: E
authors.initials: E
authors.lastname: Nomura
authors.forename: T
authors.initials: T
authors.lastname: Sakakibara
authors.forename: Y
authors.initials: Y
authors.lastname: Yamauchi
authors.forename: L H
authors.initials: LH
authors.lastname: Huang
authors.forename: M
authors.initials: M
authors.lastname: Norcia
authors.forename: L M
authors.initials: LM
authors.lastname: Wondrack
authors.forename: J A
authors.initials: JA
authors.lastname: Sutcliffe
authors.forename: N
authors.initials: N
authors.lastname: Kojima
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D002839:Chromans / Q000737:chemistry* / Q000302:isolation & purification* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000302:isolation & purification* / Q000494:pharmacology; D004926:Escherichia coli / Q000187:drug effects / Q000201:enzymology; D005285:Fermentation; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D010407:Penicillium; D059005:Topoisomerase II Inhibitors
chemical_list: D000900:Anti-Bacterial Agents; C111760:CJ 12373; D002839:Chromans; D004791:Enzyme Inhibitors; D059005:Topoisomerase II Inhibitors