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.
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.
Morishita
Y
Y
Tokyo Research Laboratories, Kyowa Hakko Kogyo Ltd, Japan.
Chiba
S
S
Tsukuda
E
E
Tanaka
T
T
Ogawa
T
T
Yamasaki
M
M
Yoshida
M
M
Kawamoto
I
I
Matsuda
Y
Y
D000595:Amino Acid Sequence; D000818:Animals; D016466:CHO Cells; D002118:Calcium / Q000378:metabolism; D002417:Cattle; D006224:Cricetinae; D003470:Culture Media; D065128:Endothelin Receptor Antagonists; D016232:Endothelins / Q000378:metabolism; D005285:Fermentation; D006801:Humans; D008168:Lung / Q000166:cytology; D008566:Membranes / Q000378:metabolism; D008969:Molecular Sequence Data; D010456:Peptides, Cyclic / Q000096:biosynthesis / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D013302:Streptomyces / Q000378:metabolism*
D003470:Culture Media; D065128:Endothelin Receptor Antagonists; D016232:Endothelins; D010456:Peptides, Cyclic; C087120:RES 701-1; D002118:Calcium