RES-1214-1 AND RES-1214-2, NOVEL NONPEPTIDIC ENDOTHELIN TYPE-A RECEPTOR ANTAGONISTS PRODUCED BY PESTALOTIOPSIS SP

Authors
OGAWA T ANDO K AOTANI Y SHINODA K TANAKA T TSUKUDA E YOSHIDA M MATSUDA Y
Citation
T. Ogawa et al., RES-1214-1 AND RES-1214-2, NOVEL NONPEPTIDIC ENDOTHELIN TYPE-A RECEPTOR ANTAGONISTS PRODUCED BY PESTALOTIOPSIS SP, Journal of antibiotics, 48(12), 1995, pp. 1401-1406
Citations number
10
Categorie Soggetti
Pharmacology & Pharmacy",Immunology,"Biothechnology & Applied Migrobiology
Journal title
Journal of antibiotics → ACNP
ISSN journal
00218820
Volume
48
Issue
12
Year of publication
1995
Pages
1401 - 1406
Database
ISI
SICI code
0021-8820(1995)48:12<1401:RARNNE>2.0.ZU;2-B
Abstract
RES-1214-1 and -2, novel and non-peptidic endothelin antagonists, were isolated from the culture broth of a fungus, Pestalotiopsis sp. RE-12 14. RES-1214-1 and -2 selectively inhibited the ET-1 binding to endoth elin type A receptor (ET(A) receptor) with IC50 values of 1.5 mu M and 20 mu M, respectively. RES-1214-1 and -2 inhibited the increase in in tracellular Ca2+ concentration elicited by 1 nM ET-1 in A10 cells. Tax onomy of producing strains, fermentation, isolation, structural determ ination, and biochemical properties of RES-1214-1 and -2 are described .