2. Academic Validation
  3. Aselacins, novel compounds that inhibit binding of endothelin to its receptor. I. The producing organism, fermentation and biological activity

Aselacins, novel compounds that inhibit binding of endothelin to its receptor. I. The producing organism, fermentation and biological activity

  • J Antibiot (Tokyo). 1994 May;47(5):523-7. doi: 10.7164/antibiotics.47.523.
M Jackson 1,  N S Burres,  J P Karwowski,  L A Alder,  P E Humphrey,  W L Kohl,  J B McAlpine
Affiliations

Affiliation

  • 1 Pharmaceutical Products Research and Development, Abbott Laboratories, Abbott Park, IL 60064.
PMID: 8040048 DOI: 10.7164/antibiotics.47.523
Abstract

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 micrograms/ml.

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