Design of Plasma Kallikrein Inhibitors : Functional and Structural Requirements of Plasma Kallikrein Inhibitors

Yuko TSUDA; Keiko WANAKA; Mayako TADA; Shosuke OKAMOTO; Akiko HIJIKATA-OKUNOMIYA; Yoshio OKADA

doi:10.1248/cpb.46.452

Yuko TSUDA, Keiko WANAKA, Mayako TADA, Shosuke OKAMOTO, Akiko HIJIKATA-OKUNOMIYA, Yoshio OKADA

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Keywords: plasma kallikrein, potent-selective inhibitor, substituted peptide, trans-4-aminomethylcyclohexanecarbonylphenylalanine-4-carboxymethylanilide

JOURNAL FREE ACCESS

1998 Volume 46 Issue 3 Pages 452-457

DOI https://doi.org/10.1248/cpb.46.452

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Abstract

The synthetic plasma kallikrein (PK) inhibitor trans-4-aminomethylcyclohexanecarbonylphenylalanine-4-carboxymethylanilide (PKSI-527) consists of three parts. Each part was replaced by analogues in an attempt to improve the potency and the selectivity of PKSI-527. Among the peptides examined, trans-4-aminomethylcyclohexanecarbonylphenylalanine-4-carboxyanilide (peptide 16) inhibited PK with a high selectivity and an IC₅₀ value of 2.7μM, being as potent as PKSI-527.

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