A new aromatase inhibitor, FR901537. I. Taxonomy, fermentation, isolation, physiochemical characteristics and biological activities

  • J Antibiot (Tokyo). 1995 Aug;48(8):757-62. doi: 10.7164/antibiotics.48.757.
N Oohata  1 ,  Y Hori ,  Y Yamagishi ,  T Fujita ,  S Takase ,  M Yamashita ,  H Terano ,  M Okuhara
Affiliations
  • 1. Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.
PMID: 7592017 DOI: 10.7164/antibiotics.48.757
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.

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