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

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...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 1998/03/15, Vol.46(3), pp.452-457
Hauptverfasser:	TSUDA, Yuko, WANAKA, Keiko, TADA, Mayako, OKAMOTO, Shosuke, HIJIKATA-OKUNOMIYA, Akiko, OKADA, Yoshio
Format:	Artikel
Sprache:	eng
Schlagworte:	Analytical, structural and metabolic biochemistry Biological and medical sciences Drug Design Enzymes and enzyme inhibitors Fundamental and applied biological sciences. Psychology Hydrolases Kallikreins - antagonists & inhibitors Kallikreins - drug effects Phenylalanine - analogs & derivatives Phenylalanine - chemical synthesis Phenylalanine - chemistry Phenylalanine - pharmacology plasma kallikrein potent-selective inhibitor Serine Proteinase Inhibitors - chemical synthesis Serine Proteinase Inhibitors - chemistry Serine Proteinase Inhibitors - pharmacology substituted peptide Tranexamic Acid - analogs & derivatives Tranexamic Acid - chemical synthesis Tranexamic Acid - chemistry Tranexamic Acid - pharmacology trans-4-aminomethylcyclohexanecarbonylphenylalanine-4-carboxymethylanilide
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Zusammenfassung:	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.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.46.452