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  • Title: Structure-based design of ketone-containing, tripeptidyl human rhinovirus 3C protease inhibitors.
    Author: Dragovich PS, Zhou R, Webber SE, Prins TJ, Kwok AK, Okano K, Fuhrman SA, Zalman LS, Maldonado FC, Brown EL, Meador JW, Patick AK, Ford CE, Brothers MA, Binford SL, Matthews DA, Ferre RA, Worland ST.
    Journal: Bioorg Med Chem Lett; 2000 Jan 03; 10(1):45-8. PubMed ID: 10636240.
    Abstract:
    Tripeptide-derived molecules incorporating C-terminal ketone electrophiles were evaluated as reversible inhibitors of the cysteine-containing human rhinovirus 3C protease (3CP). An optimized example of such compounds displayed potent 3CP inhibition activity (K = 0.0045 microM) and in vitro antiviral properties (EC50=0.34 microM) when tested against HRV serotype-14.
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