ASELACINS, NOVEL COMPOUNDS THAT INHIBIT BINDING OF ENDOTHELIN TO ITS RECEPTOR I. THE PRODUCING ORGANISM, FERMENTATION AND BIOLOGICAL ACTIVITY

MARIANNA JACKSON; NEAL S. BURRES; JAMES P. KARWOWSKI; LISA A. ALDER; PATRICK E. HUMPHREY; WILLIAM L. KOHL; JAMES B. Me ALPINE

doi:10.7164/antibiotics.47.523

ASELACINS, NOVEL COMPOUNDS THAT INHIBIT BINDING OF ENDOTHELIN TO ITS RECEPTOR

I. THE PRODUCING ORGANISM, FERMENTATION AND BIOLOGICAL ACTIVITY

MARIANNA JACKSON, NEAL S. BURRES, JAMES P. KARWOWSKI, LISA A. ALDER, PATRICK E. HUMPHREY, WILLIAM L. KOHL, JAMES B. Me ALPINE

著者情報

ジャーナルフリー

1994 年 47 巻 5 号 p. 523-527

DOI https://doi.org/10.7164/antibiotics.47.523

詳細

抄録

A radioligand test to detect inhibitors of endothelin-1 binding to its receptors in bovine atrial and porcine cerebral membranes was used to screen fungal metabolites from stationary fermentations. Inhibitory activity, observed in culture extracts of two Acremonium species, led to the discovery of aselacins A, B and C. Aselacin A inhibits binding to both membrane fractions with IC₅₀s of approximately 20 μg/ml.

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