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氨基酸与肽。二十八。与水蛭素c相关的肽片段的合成及其结构与对人白细胞弹性蛋白酶、组织蛋白酶G和α-胰凝乳蛋白酶作用之间关系的研究。

Amino acids and peptides. XXVIII. Synthesis of peptide fragments related to eglin c and studies on the relationship between their structure and effects on human leukocyte elastase, cathepsin G and alpha-chymotrypsin.

作者信息

Tsuboi S, Nakabayashi K, Matsumoto Y, Teno N, Tsuda Y, Okada Y, Nagamatsu Y, Yamamoto J

机构信息

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

出版信息

Chem Pharm Bull (Tokyo). 1990 Sep;38(9):2369-76. doi: 10.1248/cpb.38.2369.

Abstract

Various peptide fragments related to eglin c, which consists of 70 amino acid residues, were synthesized by a conventional solution method and their inhibitory effects on leukocyte elastase, cathepsin G and alpha-chymotrypsin were examined. Among them, H-Arg-Glu-Tyr-Phe-OMe (eglin c 22-25) and H-Ser-Pro-Val-Thr-Leu-Asp-Leu-Arg-Tyr-OMe (eglin c 41-49) inhibited cathepsin G and alpha-chymotrypsin but not leukocyte elastase, while H-Thr-Asn-Val-Val-OMe (eglin c 60-63) inhibited leukocyte elastase but not cathepsin G or alpha-chymotrypsin, although eglin c potently inhibited leukocyte elastase, cathepsin G and alpha-chymotrypsin. These results indicated that the interaction sites of eglin c with leukocyte elastase, cathepsin G and alpha-chymotrypsin might be different.

摘要

通过传统的溶液法合成了与由70个氨基酸残基组成的水蛭素c相关的各种肽片段,并检测了它们对白细胞弹性蛋白酶、组织蛋白酶G和α-糜蛋白酶的抑制作用。其中,H-Arg-Glu-Tyr-Phe-OMe(水蛭素c 22-25)和H-Ser-Pro-Val-Thr-Leu-Asp-Leu-Arg-Tyr-OMe(水蛭素c 41-49)抑制组织蛋白酶G和α-糜蛋白酶,但不抑制白细胞弹性蛋白酶,而H-Thr-Asn-Val-Val-OMe(水蛭素c 60-63)抑制白细胞弹性蛋白酶,但不抑制组织蛋白酶G或α-糜蛋白酶,尽管水蛭素c能有效抑制白细胞弹性蛋白酶、组织蛋白酶G和α-糜蛋白酶。这些结果表明,水蛭素c与白细胞弹性蛋白酶、组织蛋白酶G和α-糜蛋白酶的相互作用位点可能不同。

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