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

Y Morishita; S Chiba; E Tsukuda; T Tanaka; T Ogawa; M Yamasaki; M Yoshida; I Kawamoto; Y Matsuda

doi:10.7164/antibiotics.47.269

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

J Antibiot (Tokyo). 1994 Mar;47(3):269-75. doi: 10.7164/antibiotics.47.269.

Authors

Y Morishita¹, S Chiba, E Tsukuda, T Tanaka, T Ogawa, M Yamasaki, M Yoshida, I Kawamoto, Y Matsuda

Affiliation

¹ Tokyo Research Laboratories, Kyowa Hakko Kogyo Ltd, Japan.

PMID: 8175478
DOI: 10.7164/antibiotics.47.269

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.

MeSH terms

Amino Acid Sequence
Animals
CHO Cells
Calcium / metabolism
Cattle
Cricetinae
Culture Media
Endothelin Receptor Antagonists*
Endothelins / metabolism
Fermentation
Humans
Lung / cytology
Membranes / metabolism
Molecular Sequence Data
Peptides, Cyclic* / biosynthesis
Peptides, Cyclic* / chemistry
Peptides, Cyclic* / isolation & purification
Peptides, Cyclic* / pharmacology
Streptomyces / metabolism*

Substances

Culture Media
Endothelin Receptor Antagonists
Endothelins
Peptides, Cyclic
RES 701-1
Calcium