Amino Acids and Peptides. XVI. Synthesis of N-Terminal Tetrapeptide Analogs of Fibrin α-Chain and Their Inhibitory Effects on Fibrinogen : Thrombin Clotting

N-Terminal tetrapeptide analogs of fibrin α-chain were synthesized by the solution method using a new active ester, the ester of the oxime of p-nitroacetophenone, and by the solid-phase method. Their inhibitory effects on fibrinogen/thrombin clotting were examined. Of the synthetic peptides, amide a...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 1992/12/25, Vol.40(12), pp.3253-3260
Hauptverfasser:	KAWASAKI, Koichi, HIRASE, Katsuhiko, MIYANO, Masanori, TSUJI, Toshiki, IWAMOTO, Masanori
Format:	Artikel
Sprache:	eng
Schlagworte:	active ester Amino Acid Sequence anticoagulant Anticoagulants - chemical synthesis Anticoagulants - pharmacology Blood Coagulation - drug effects Chemistry Exact sciences and technology fibrin α-chain Fibrinogen - antagonists & inhibitors fibrinogen/thrombin clotting Fibrinopeptide A - chemical synthesis Fibrinopeptide A - pharmacology Humans Molecular Sequence Data Oligopeptides - chemical synthesis Oligopeptides - pharmacology Organic chemistry Peptide Fragments - chemical synthesis Peptide Fragments - pharmacology peptide synthesis Peptides Preparations and properties Protein Conformation Structure-Activity Relationship Thrombin - antagonists & inhibitors
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Zusammenfassung:	N-Terminal tetrapeptide analogs of fibrin α-chain were synthesized by the solution method using a new active ester, the ester of the oxime of p-nitroacetophenone, and by the solid-phase method. Their inhibitory effects on fibrinogen/thrombin clotting were examined. Of the synthetic peptides, amide analogs of Gly-Pro-Arg-Pro exhibited a more potent inhibitory effect.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.40.3253