RES-701-1, A NOVEL AND SELECTIVE ENDOTHELIN TYPE-B RECEPTOR ANTAGONIST PRODUCED BY STREPTOMYCES SP RE-701 .1. CHARACTERIZATION OF PRODUCINGSTRAIN, FERMENTATION, ISOLATION, PHYSICOCHEMICAL AND BIOLOGICAL PROPERTIES

Citation
Y. Morishita et al., RES-701-1, A NOVEL AND SELECTIVE ENDOTHELIN TYPE-B RECEPTOR ANTAGONIST PRODUCED BY STREPTOMYCES SP RE-701 .1. CHARACTERIZATION OF PRODUCINGSTRAIN, FERMENTATION, ISOLATION, PHYSICOCHEMICAL AND BIOLOGICAL PROPERTIES, Journal of antibiotics, 47(3), 1994, pp. 269-275
Citations number
14
Categorie Soggetti
Pharmacology & Pharmacy",Immunology
Journal title
ISSN journal
00218820
Volume
47
Issue
3
Year of publication
1994
Pages
269 - 275
Database
ISI
SICI code
0021-8820(1994)47:3<269:RANASE>2.0.ZU;2-1
Abstract
RES-701-1, a novel cyclic peptide endothelin antagonist, was isolated from the culture broth of Streptomyces sp. RE-701. RES-701-1 selective ly inhibited the ET-1 binding to type B endothelin receptor (ET(B) rec eptor) with an IC50 of 10 nM expressed in CHO cells and blocked the ET -1-induced elevation of intracellular free Ca2+ concentration in ET(B) receptor-expressing COS-7 cells. Characterization of producing strain , fermentation, isolation, structure, physico-chemical and biological properties of RES-701-1 are described.