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

被引：11

作者：

JACKSON, M

BURRES, NS

KARWOWSKI, JP

ALDER, LA

HUMPHREY, PE

KOHL, WL

MCALPINE, JB

机构：

[1] Pharmaceutical Products Research and Development, Abbott Laboratories, IL 60064, Abbott Park

来源：

JOURNAL OF ANTIBIOTICS | 1994年 / 47卷 / 05期

关键词：

D O I：

10.7164/antibiotics.47.523

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

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 IC(50)s of approximately 20 mu g/ml.

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页码：523 / 527

页数：5

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