RES-701-1，一种由链霉菌属RE-701产生的新型选择性内皮素B型受体拮抗剂。I. 产生菌的特性、发酵、分离、理化性质及生物学特性
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.
作者信息
Morishita Y, Chiba S, Tsukuda E, Tanaka T, Ogawa T, Yamasaki M, Yoshida M, Kawamoto I, Matsuda Y
机构信息
Tokyo Research Laboratories, Kyowa Hakko Kogyo Ltd, Japan.
出版信息
J Antibiot (Tokyo). 1994 Mar;47(3):269-75. doi: 10.7164/antibiotics.47.269.
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.
RES-701-1是一种新型环肽内皮素拮抗剂，从链霉菌属RE-701的培养液中分离得到。RES-701-1能选择性抑制ET-1与B型内皮素受体（ETB受体）的结合，在CHO细胞中其IC50为10 nM，并能阻断ET-1诱导的表达ETB受体的COS-7细胞内游离Ca2+浓度的升高。本文描述了RES-701-1产生菌的特性、发酵、分离、结构、理化性质及生物学特性。
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