RES-701-1,a novel and selective endothelin type B receptor antagonist produced by streptomyces sp. RE-701. I. Characterization of producing strain, fermentation, isolation, physico-chemical and biological properties

Abstract

RES-701-1, a novel cyclic peptide endothelin antagonist, was isolated from the culture broth of Streptomyces sp. RE-701. RES-701-1 selectively inhibited the ET-1 binding to type B endothelin receptor (ETB receptor) with an IC50 of 10 nM expressed in CHO cells and blocked the ET-1-induced elevation of intracellular free Ca2+ concentration in ETB receptor-expressing COS-7 cells. Characterization of producing strain, fermentation, isolation, structure, physico-chemical and biological properties of RES-701-1 are described. © 1994, JAPAN ANTIBIOTICS RESEARCH ASSOCIATION. All rights reserved.