ASELACINS, NOVEL COMPOUNDS THAT INHIBIT BINDING OF ENDOTHELIN TO ITS RECEPTOR .1. THE PRODUCING ORGANISM, FERMENTATION AND BIOLOGICAL-ACTIVITY

Authors
JACKSON M BURRES NS KARWOWSKI JP ALDER LA HUMPHREY PE KOHL WL MCALPINE JB
Citation
M. Jackson et al., ASELACINS, NOVEL COMPOUNDS THAT INHIBIT BINDING OF ENDOTHELIN TO ITS RECEPTOR .1. THE PRODUCING ORGANISM, FERMENTATION AND BIOLOGICAL-ACTIVITY, Journal of antibiotics, 47(5), 1994, pp. 523-527
Citations number
15
Categorie Soggetti
Pharmacology & Pharmacy",Immunology
Journal title
Journal of antibiotics → ACNP
ISSN journal
00218820
Volume
47
Issue
5
Year of publication
1994
Pages
523 - 527
Database
ISI
SICI code
0021-8820(1994)47:5<523:ANCTIB>2.0.ZU;2-2
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 a ctivity, observed in culture extracts of two Acremonium species, led t o the discovery of aselacins A, B and C. Aselacin A inhibits binding t o both membrane fractions with IC(50)s of approximately 20 mu g/ml.