C-terminal modifications of an endothelin antagonist RES-701-1: Production of ET/ET dual selective analogs.

Autor: Shibata, Kenji, Yano, Keiichi, Tanaka, Takeo, Matsuda, Yuzuru, Yamasaki, Motoo
Zdroj: Letters in Peptide Science; Jun1997, Vol. 4 Issue 3, p167-170, 4p
Abstrakt: RES-701-1 is an endothelin B receptor (ET) selective peptidic antagonist, which has a novel cyclic structure of microbial origin. Modification at the C-terminal free carboxyl group of RES-701-1 by a methyl ester results in an ET/ET dual selective analog, which showed relatively high affinity for ET receptor subtype, while retaining the affinity for ET. The carboxyl-group-deleted analog with tryptamine as the C-terminal residue also showed relatively weak affinity for ET; however, benzyl ester or amide analogs did not show remarkable affinity for ET. It is suggested that the binding mode of RES-701-1 and its analogs is different from those of known ligands for ET receptors. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index