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.
MeSH terms
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Animals
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Aromatase / metabolism
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Aromatase Inhibitors*
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Bacillus
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Cattle
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Female
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Fermentation
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Humans
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Mice
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Naphthols / chemistry
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Naphthols / isolation & purification*
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Naphthols / pharmacology*
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Ovary / drug effects
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Ovary / enzymology
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Pantetheine / analogs & derivatives*
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Pantetheine / chemistry
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Pantetheine / isolation & purification
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Pantetheine / pharmacology
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Placenta / drug effects
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Placenta / enzymology
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Rats
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Rats, Wistar
Substances
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Aromatase Inhibitors
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Naphthols
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FR 901537
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Pantetheine
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Aromatase