A New Aromatase Inhibitor, FR901537: I. Taxonomy, Fermentation, Isolation, Physicochemical 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,...

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Bibliographic Details
Published in:Journal of antibiotics 1995/08/25, Vol.48(8), pp.757-762
Main Authors: OOHATA, NOBUTAKA, HORI, YASUHIRO, YAMAGISHI, YUKIKO, FUJITA, TAKASHI, TAKASE, SHIGEHIRO, YAMASHITA, MICHIO, TERANO, HIROSHI, OKUHARA, MASAKUNI
Format: Article
Language:English
Subjects:
Antineoplastic agents
Bacillus
Biological and medical sciences
Chemotherapy
Medical sciences
Pharmacology. Drug treatments
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Summary: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 11β-hydroxylase from bovine adrenal cortex. Lineweaver-Burk plot analysis revealed that FR901537 is a competitive inhibitor.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.48.757