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Guay D, Beaulieu C, Percival MD: Therapeutic Utility and Medicinal Chemistry of Cathepsin C Inhibitors. . Curr Top Med Chem. 2010 Mar 26.
Cathepsin C null mice and humans with Cat C loss of function mutations (Papillon-Lefevre syndrome) show deficiencies in disease-relevant proteases including neutrophil elastase, cathepsin G, chymases and granzymes and the Cat C mice are protected in a number of disease models.
Nearly all potent and selective Cat C inhibitors described are based on the preferred dipeptide substrates bearing either irreversible (e.g. diazomethylketone, acyloxymethyl ketone, o-acyl hydroxamic acid and vinyl sulfone) or reversible (e.g. semicarbazide, nitrile and cyanamide) electrophilic warheads. |
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