Synthesis of stereoisomeric Suc-Tyr-Leu-Val-pNA and their properties as substrate and inhibitor for human spleen fibrinolytic proteinase (SFP).
作者:YOSHIO OKADA、YUKO TSUDA、YOKO NAGAMATSU、UTAKO OKAMOTO
DOI:10.1248/cpb.29.1483
日期:——
Stereoisomeric analogues of Suc-Tyr-Leu-Val-pNA were synthesized in the conventional manner and their properties as the substrate and/or the inhibitor against human spleen fibrinolytic proteinase (SFP) were tested. Suc-D-Tyr-L-Leu-L-Val-pNA (II) was hydrolyzed to release p-nitroaniline with Keat/Km value (3700), whereas Keat/Km value of Suc-L-Tyr-L-Leu-L-Val-pNA (I) was 22647. Suc-L-Tyr-D-Leu-D-Val-pNA (III) inhibited the hydrolytic activity of SFP towards both the peptide (I) and fibrin.
按常规方法合成了 Suc-Tyr-Leu-L-Val-pNA 的立体异构体类似物,并测试了它们作为人脾纤维蛋白溶解酶(SFP)底物和/或抑制剂的特性。Suc-D-Tyr-L-Leu-L-Val-pNA (II) 被水解后释放出对硝基苯胺,Keat/Km 值为 3700,而 Suc-L-Tyr-L-Leu-L-Val-pNA (I) 的 Keat/Km 值为 22647。Suc-L-Tyr-D-Leu-D-Val-pNA (III) 可抑制 SFP 对多肽 (I) 和纤维蛋白的水解活性。