RES-1214-1 and -2, novel non-peptidic endothelin type A receptor antagonists produced by Pestalotiopsis sp.
RES-1214-1 and -2, novel and non-peptidic endothelin antagonists, were isolated from the cultured broth of a fungus, Pestalotiopsis sp. RE-1214. RES-1214-1 and -2 selectivity inhibited the ET-1 binding to endothelin type A receptor (ETA receptor) with IC50 values of 1.5 microM and 10 microM, respectively. RES-1214-1 and -2 inhibited the increase in intracellular Ca2+ concentration elicited by 1 nM ET-1 in A10 cells. Taxonomy of producing strains, fermentation, isolation, structural determination, and biochemical properties of RES-1214-1 and-2 are described.
Ogawa
T
T
Tokyo Research Laboratories, Kyowa Hakko Kogyo Co, Ltd, Japan.
Ando
K
K
Aotani
Y
Y
Shinoda
K
K
Tanaka
T
T
Tsukuda
E
E
Yoshida
M
M
Matsuda
Y
Y
D000818:Animals; D002417:Cattle; D002460:Cell Line; D065128:Endothelin Receptor Antagonists; D062425:Hydroxybenzoate Ethers; D062385:Hydroxybenzoates / Q000737:chemistry / Q000494:pharmacology*; D003904:Mitosporic Fungi / Q000378:metabolism*; D015394:Molecular Structure; D010647:Phenyl Ethers / Q000737:chemistry / Q000494:pharmacology*; D011869:Radioligand Assay; D044022:Receptor, Endothelin A; D013057:Spectrum Analysis
D065128:Endothelin Receptor Antagonists; D062425:Hydroxybenzoate Ethers; D062385:Hydroxybenzoates; D010647:Phenyl Ethers; C097792:RES 1214-1; C097793:RES 1214-2; D044022:Receptor, Endothelin A