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Trifluoroacetyl tripeptides as potent inhibitors of human leukocyte elastase.

作者:Patrick P. Lestienne, Jean Luc Dimicoli, Joseph G. Bieth · 发表于:Journal of Biological Chemistry · 年份:1977 · DOI:10.1016/s0021-9258(17)40005-6 · 被引用次数:11 · 研究领域:Protease and Inhibitor Mechanisms、Peptidase Inhibition and Analysis、Cell Adhesion Molecules Research

Trifluoroacetylated peptides are much more potent inhibitors of human leukocyte elastase than the corresponding unblocked, acylated or benzyloxycarbonylated peptides. The most active compound was trifluoroacetyl-Val-Tyr-Val (Ki = 1.3 micron). A number of free and NH2-terminal-substituted peptides exhibited similar affinities for porcine pancreatic and human leukocyte elastase, indicating that these two enzymes must have similar specificity sites.