title: A new aromatase inhibitor, FR901537. I. Taxonomy, fermentation, isolation, physiochemical characteristics and biological activities.
abstract: FR901537 is a new aromatase inhibitor produced by a bacterium Bacillus sp. No. 3072. Structural studies of FR901537 suggested that it was a novel naphthol derivative having pantetheine in its structure. FR901537 showed a potent inhibitory activity against aromatase from human placenta or rat ovary, but did not inhibit the activity of 11 beta-hydroxylase from bovine adrenal cortex. Lineweaver-Burk plot analysis revealed that FR901537 is a competitive inhibitor.
authors.affiliation: Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.
authors.forename: N
authors.initials: N
authors.lastname: Oohata
authors.forename: Y
authors.initials: Y
authors.lastname: Hori
authors.forename: Y
authors.initials: Y
authors.lastname: Yamagishi
authors.forename: T
authors.initials: T
authors.lastname: Fujita
authors.forename: S
authors.initials: S
authors.lastname: Takase
authors.forename: M
authors.initials: M
authors.lastname: Yamashita
authors.forename: H
authors.initials: H
authors.lastname: Terano
authors.forename: M
authors.initials: M
authors.lastname: Okuhara
mesh_terms: D000818:Animals; D001141:Aromatase / Q000378:metabolism; D047072:Aromatase Inhibitors; D001407:Bacillus; D002417:Cattle; D005260:Female; D005285:Fermentation; D006801:Humans; D051379:Mice; D009284:Naphthols / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D010053:Ovary / Q000187:drug effects / Q000201:enzymology; D010204:Pantetheine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D010920:Placenta / Q000187:drug effects / Q000201:enzymology; D051381:Rats; D017208:Rats, Wistar
chemical_list: D047072:Aromatase Inhibitors; D009284:Naphthols; C096595:FR 901537; D010204:Pantetheine; D001141:Aromatase