Synthesis of Tripeptide Chloromethyl Ketones and Examination of Their Inhibitory Effects on Plasmin and Plasma Kallikrein

With the aim of obtaining selective synthetic inhibitors of plasmin and plasma kallikrein, D-Ile-Phe-Lys-CH2Cl, Ile-Phe-Lys-CH2Cl, D-Ile-Phe-Arg-CH2Cl and Ile-Phe-Arg-CH2Cl were synthesized and their inhibitory activity against plasmin, plasma kallikrein and other trypsin-like serine proteinases was...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 1989/11/25, Vol.37(11), pp.3108-3111
Hauptverfasser:	TSUDA, Yuko, TENO, Naoki, OKADA, Yoshio, WANAKA, Keiko, BOHGAKI, Miyako, HIJIKATA-OKUNOMIYA, Akiko, OKAMOTO, Utako, NAITO, Taketoshi, OKAMOTO, Shosuke
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Chloromethyl Ketones - chemical synthesis Amino Acid Sequence Analytical, structural and metabolic biochemistry Biological and medical sciences Chemical Phenomena chemical synthesis Chemistry chloromethyl ketone derivative Depression, Chemical Enzymes and enzyme inhibitors Fibrinolysin - antagonists & inhibitors Fibrinolysin - metabolism Fundamental and applied biological sciences. Psychology Hydrolases Kallikreins - antagonists & inhibitors Kallikreins - blood Molecular Sequence Data plasma kallikrein plasmin selective inhibitor substrate-derived inhibitor synthetic inhibitor trypsin-like serine proteinase
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Beschreibung
Zusammenfassung:	With the aim of obtaining selective synthetic inhibitors of plasmin and plasma kallikrein, D-Ile-Phe-Lys-CH2Cl, Ile-Phe-Lys-CH2Cl, D-Ile-Phe-Arg-CH2Cl and Ile-Phe-Arg-CH2Cl were synthesized and their inhibitory activity against plasmin, plasma kallikrein and other trypsin-like serine proteinases was examined. Among them, D-Ile-Phe-Arg-CH2Cl exhibited a highly selective inhibitory activity against plasma kallikrein, yet D-Ile-Phe-Lys-CH2Cl exhibited nearly the same order of inhibitory activity against plasmin as well as plasma kallikren.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.37.3108