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C-terminal modifications of an endothelin antagonist RES-701-1: Production of ETA/ETB dual selective analogs
Authors:Shibata  Kenji  Yano  Keiichi  Tanaka  Takeo  Matsuda  Yuzuru  Yamasaki  Motoo
Institution:(1) Tokyo Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., 3-6-6 Asahi-machi, 194 Machida-shi, Tokyo, Japan
Abstract:Summary RES-701-1 is an endothelin B receptor (ETB) 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 ETA/ETB dual selective analog, which showed relatively high affinity for ETA receptor subtype, while retaining the affinity for ETB. The carboxyl-group-deleted analog with tryptamine as the C-terminal residue also showed relatively weak affinity for ETA; however, benzyl ester or amide analogs did not show remarkable affinity for ETA. It is suggested that the binding mode of RES-701-1 and its analogs is different from those of known ligands for ET receptors.
Keywords:Cyclic peptide  Receptor  Subtype  Endothelin  Antagonist
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