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Linear peptide ETA antagonists: rational design and practical derivatization of N-terminal amino- and imino-carbonylated tripeptide derivatives by Toshio Nagase; Toshiaki Mase; Takehiro Fukami; Takashi Hayama; Kagari Fujita; Kenji Niiyama; Hirobumi Takahashi; Uno Kumagai; Yuko Urakawa; Yohko Nagasawa; Masaki Ihara; Masaru Nishikibe; Kiyofumi Ishikawa is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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Novel linear tripeptides possessing high endothelin antagonist activity were derived from endothelin antagonistic cyclic pentapeptides represented by BQ-123. The N-terminal urea moiety of the linear tripeptide derivatives was essential to show the strong antagonist activity. An easy method to prepare these peptides by treatment of the corresponding N-phenoxycarbonylated tripeptide esters with primary or secondary amines is described. In the course of chemical modification of the endothelin (ET) antagonistic cyclic pentapeptide (CPP) BE-18257A (1) of microbial origin, we found that a series of novel CPPs represented by BQ-123 (2) showed antagonism that was potent and highly selective for ETA receptors. 2 Detailed investigations of structure-activity relationships in these CPPs revealed that peptides possessing various kinds of the third amino acid residue (Xxx in 3) all had similar ETA antagonistic activity) These results suggested that the residue did not directly interact with endothelin receptors but worked to maintain a suitable conformation and/or configuration of CPPs for exhibiting antagonistic activity. We therefore attempted to generate linear peptide ET antagonists which l

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Author

Toshio Nagase; Toshiaki Mase; Takehiro Fukami; Takashi Hayama; Kagari Fujita; Kenji Niiyama; Hirobumi Takahashi; Uno Kumagai; Yuko Urakawa; Yohko Nagasawa; Masaki Ihara; Masaru Nishikibe; Kiyofumi Ishikawa

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)

Published

1995

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)