207514-59-8Relevant articles and documents
Design of plasma kallikrein inhibitors: Functional and structural requirements of plasma kallikrein inhibitors
Tsuda, Yuko,Wanaka, Keiko,Tada, Mayako,Okamoto, Shosuke,Hijikata-Okunomiya, Akiko,Okada, Yoshio
, p. 452 - 457 (2007/10/03)
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.