Amino acids and peptides. XXX. Synthesis of eglin c(41-49) and eglin c(60-63) and examination of their inhibitory activity towards human leukocyte elastase, cathepsin G, porcine pancreatic elastase and .ALPHA.-chymotrypsin.
作者:Satoshi TSUBOI、Miho TAKEDA、Yoshio OKADA、Yoko NAGAMATSU、Junichiro YAMAMOTO
DOI:10.1248/cpb.39.184
日期:——
H-Ser-Pro-Val-Thr-Leu-Asp-Leu-Arg-Tyr-OH and H-Thr-Asn-Val-Val-OH, which correspond to the sequences 41-49 and 60-63 of eglin c, respectively, were synthesized by a conventional solution approach using the newly developed 6-chloro-2-pyridyl ester method. The inhibitory activities of the above two peptides against human leukocyte elastase, cathepsin G, porcine pancreatic elastase and α-chymotrypsin were examined in comparison with those of the corresponding methyl esters.
H-Ser-Pro-Val-Thr-Leu-Asp-Leu-Arg-Tyr-OH 和 H-Thr-Asn-Val-Val-OH 分别对应于 eglin c 的序列 41-49 和 60-63,通过采用新开发的 6-氯-2-吡啶酯方法,使用常规溶液法合成。以上两种肽对人类白细胞弹性蛋白酶、半胱天冬酶 G、猪胰弹性蛋白酶和 α-化学蛋白酶的抑制活性进行了比较,分析其与相应甲基酯的活性差异。