Design of plasma kallikrein inhibitors: Functional and structural requirements of plasma kallikrein inhibitors

DOI: 10.1248/cpb.46.452

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 452 - 457 (1998)

Update date:2022-08-04

Topics:

Authors:

Tsuda, Yuko

Wanaka, Keiko

Tada, Mayako

Okamoto, Shosuke

Hijikata-Okunomiya, Akiko

Okada, Yoshio

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Article abstract of DOI:10.1248/cpb.46.452

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-aminomethyl-cyclohexanecarbonylphenylalanine-4- carboxyanilide (peptide 16) inhibited PK with a high selectivity and an IC₅₀ value of 2.7 μM, being as potent as PKSI-527.

Full text of DOI:10.1248/cpb.46.452

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