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.

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