title: Design of plasma kallikrein inhibitors: functional and structural requirements of plasma kallikrein inhibitors.
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.
authors.affiliation: Faculty of Pharmaceutical Sciences, Kobe Gakuin University, Nishi-ku, Japan.
authors.forename: Y
authors.initials: Y
authors.lastname: Tsuda
authors.forename: K
authors.initials: K
authors.lastname: Wanaka
authors.forename: M
authors.initials: M
authors.lastname: Tada
authors.forename: S
authors.initials: S
authors.lastname: Okamoto
authors.forename: A
authors.initials: A
authors.lastname: Hijikata-Okunomiya
authors.forename: Y
authors.initials: Y
authors.lastname: Okada
mesh_terms: D015195:Drug Design; D007610:Kallikreins / Q000037:antagonists & inhibitors* / Q000187:drug effects; D010649:Phenylalanine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015842:Serine Proteinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D014148:Tranexamic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D015842:Serine Proteinase Inhibitors; C064866:PKSI 527; D010649:Phenylalanine; D014148:Tranexamic Acid; D007610:Kallikreins