A new aromatase inhibitor, FR901537. I. Taxonomy, fermentation, isolation, physiochemical characteristics and biological activities.
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.
Oohata
N
N
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.
Hori
Y
Y
Yamagishi
Y
Y
Fujita
T
T
Takase
S
S
Yamashita
M
M
Terano
H
H
Okuhara
M
M
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
D047072:Aromatase Inhibitors; D009284:Naphthols; C096595:FR 901537; D010204:Pantetheine; D001141:Aromatase