氨基酸与肽。十六。纤维蛋白α链N端四肽类似物的合成及其对纤维蛋白原/凝血酶凝血的抑制作用。

Amino acids and peptides. XVI. Synthesis of N-terminal tetrapeptide analogs of fibrin alpha-chain and their inhibitory effects on fibrinogen/thrombin clotting.

作者信息

Kawasaki K, Hirase K, Miyano M, Tsuji T, Iwamoto M

机构信息

Faculty of Pharmaceutical Sciences, Kobe-Gakuin University, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1992 Dec;40(12):3253-60. doi: 10.1248/cpb.40.3253.

DOI:10.1248/cpb.40.3253

PMID:1294328

Abstract

N-Terminal tetrapeptide analogs of fibrin alpha-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.

摘要

采用新的活性酯（对硝基苯乙酮肟酯）通过溶液法和固相法合成了纤维蛋白α链的N端四肽类似物。检测了它们对纤维蛋白原/凝血酶凝血的抑制作用。在合成肽中，甘氨酰-脯氨酰-精氨酰-脯氨酸的酰胺类似物表现出更强的抑制作用。