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  • Title: Design of plasma kallikrein inhibitors: functional and structural requirements of plasma kallikrein inhibitors.
    Author: Tsuda Y, Wanaka K, Tada M, Okamoto S, Hijikata-Okunomiya A, Okada Y.
    Journal: Chem Pharm Bull (Tokyo); 1998 Mar; 46(3):452-7. PubMed ID: 9549887.
    Abstract:
    The synthetic plasma kallikrein (PK) inhibitor trans-4-aminomethylcyclohexanecarbonylphenylalanine-4-carboxyme thylanilide (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-carboxyan ilide (peptide 16) inhibited PK with a high selectivity and an IC50 value of 2.7 microM, being as potent as PKSI-527.
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