THE JOURNAL OF ANTIBIOTICS RES-1149-1 and -2, Novel Non-peptidic Endothelin Type B Receptor Antagonists Produced by Aspergillus sp. I. Taxonomy of Producing Strain, Fermentation, Isolation, and Physico-chemical and Biological Properties
نویسندگان
چکیده
RES-1149-1 and -2, novel and non-peptidic endothelin antagonists, were isolated from the cultured broth of a fungus, Aspergillus sp. RE-1 149. RES-1 149-1 and -2 selectively inhibited the ET-1 binding to endothelin type B receptor (ETB receptor) with IC50 values of 1.5pM and 20//M, respectively. Taxonomyof producing strains, fermentation, isolation, and physico-chemical properties of RES-1149-1 and -2 are described.
منابع مشابه
RES-1149-1 and -2, novel non-peptidic endothelin type B receptor antagonists produced by Aspergillus sp. II. Structure determination and derivatization.
The structures of two novel non-peptidic endothelin type B receptor antagonists, RES-1149-1 and -2 were determined by spectroscopic methods. Several derivatives were synthesized from RES-1149-1 for biological assay.
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RES-1149-1 and -2, produced by Aspergillus sp. RE-1149, were found to be non-peptidic antagonists for endothelin type B receptor (ET(B) receptor). RES-1149-1 and -2 selectively inhibited the endothelin-1 (ET-1) binding to ET(B) receptor in a competitive manner with IC50 values of 1.5 microM and 20 microM, respectively. RES-1149-1 inhibited the increase in intracellular Ca2+ concentration elicit...
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