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  • Title: Novel aza peptide inhibitors and active-site probes of papain-family cysteine proteases.
    Author: Verhelst SH, Witte MD, Arastu-Kapur S, Fonovic M, Bogyo M.
    Journal: Chembiochem; 2006 Jun; 7(6):943-50. PubMed ID: 16607671.
    Abstract:
    Recent characterization of multiple classes of functionalized azapeptides as effective covalent inhibitors of cysteine proteases prompted us to investigate O-acyl hydroxamates and their azapeptide analogues for use as activity-based probes (ABPs). We report here a new class of azaglycine-containing O-acylhydroxamates that form stable covalent adducts with target proteases. This allows them to be used as ABPs for papain family cysteine proteases. A second class of related analogues containing a novel O-acyl hydroxyurea warhead was found to function as covalent inhibitors of papain-like proteases. These inhibitors can be easily synthesized on solid support, which allows rapid optimization of compounds with improved selectivity and potency for a given target enzyme. We present here one such optimized inhibitor that showed selective inhibition of falcipain 1, a protease of the malaria-causing parasite, Plasmodium falciparum.
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