RES-1149-1 and -2, novel non-peptidic endothelin type B receptor antagonists produced by Aspergillus sp. II. Structure determination and derivatization.
نویسندگان
چکیده
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.
منابع مشابه
RES-1149-1 and -2, novel non-peptidic endothelin type B receptor antagonists produced by Aspergillus sp. III. Biochemical properties of RES-1149-1, -2 and structure-activity relationships.
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...
متن کاملTHE 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
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...
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Endothelins (ETs) are a family of potent vasoactive peptides found in at least three distinct isoforms: ET-1, ET-2, and ET-31}. Two major subtypes of endothelin receptors, termed ETAand ETB, have been identified in various target cells2). It is well known that ETs act on these G protein-coupled receptors and exert multiple pharmacological effects3). As the development of potent and selective en...
متن کاملRES-701-2, -3 and -4, novel and selective endothelin type B receptor antagonists produced by Streptomyces sp. I. Taxonomy of producing strains, fermentation, isolation, and biochemical properties.
RES-701-2, -3 and -4, novel cyclic peptide endothelin antagonists, were isolated from the culture broths of Streptomyces sp. RE-701 and RE-896, RES-701s selectively inhibited the ET-1 binding to endothelin type B receptor (ETB receptor) with IC50 values ranging from 5 to 20 nM. Taxonomy of the producing strains, fermentation, isolation and biochemical properties of RES-701s are described.
متن کاملStachybocins, novel endothelin receptor antagonists, produced by Stachybotrys sp. M6222. II. Structure determination of stachybocins A, B and C.
The structures of stachybocins A, B and C, new endothelin receptor antagonist, were determined by NMR spectral analysis using pulse-field-gradient technique. Stachybocin A consists of two spirobenzofuran units each fused to a substituted decalin, which were connected by a lysine residue. Stachybocins B and C are derivatives of stachybocin A with an additional hydroxy group at the same position ...
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ورودعنوان ژورنال:
- The Journal of antibiotics
دوره 49 1 شماره
صفحات -
تاریخ انتشار 1996