In vitro inhibition of Pseudomonas aeruginosa elastase by metal-chelating peptide derivatives.

Infection and Immunity
E KesslerS Blumberg


Pseudomonas aeruginosa elastase is a zinc metalloendopeptidase, probably responsible for the tissue destruction observed during infections with this organism. The elastase of a virulent Pseudomonas aeruginosa strain (Habs serotype 1) was isolated and found to have a molecular weight of 35,000; it readily degraded elastin and cartilage proteoglycans. A series of amino acid and peptide derivatives containing the metal-chelating moieties hydroxamate, phosphoryl, or thiol were synthesized and tested as potential inhibitors of the enzyme. Inhibition constants (K(i)s) for the compounds were determined with the chromophoric substrate furylacryloyl-glycyl-l-leucyl-l-alanine. The hydroxamic acid derivatives of benzyloxycarbonyl-glycine, benzyloxycarbonyl-l-leucine and benzyloxycarbonyl-l-phenylalanine had inhibition constants in the range of 11 to 28 muM. The 2-mercaptoacetyl derivatives of l-leucyl-d-phenylalanine and l-leucyl-l-phenylalanine had K(i) values of 34 and 1.5 muM, respectively, demonstrating the stereospecificity of the inhibition. The most potent inhibitors tested were 2- mercaptoacetyl-l-phenylalanyl-l-leucine and phosphoryl-l-leucyl-l-phenylala-nine (K(i) = 0.2 muM). Similar compounds lacking the metal-chelating moiety ...Continue Reading


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