Identification of a New Class of Nonpeptidic Inhibitors of Cruzain
Brak K, Doyle PS, McKerrow JH, Ellman JA. Identification of a New Class of Nonpeptidic Inhibitors of Cruzain. Journal Of The American Chemical Society 2008, 130: 6404-6410. PMID: 18435536, PMCID: PMC2765048, DOI: 10.1021/ja710254m.Peer-Reviewed Original ResearchConceptsVinyl sulfonesNonpeptidic inhibitorsAdditional binding interactionsStructure-based designMajor cysteine proteaseMammalian cell cultureChagas diseasePotent nonpeptidic inhibitorsCruzain inhibitorsT. cruzi parasiteCruzain inhibitionCruzainCysteine proteasesBinding interactionsProtease substratesS3 pocketTrypanosoma cruziPeptidic inhibitorsCruzi parasitesMechanistic insightsNew chemotherapeuticsCleavage efficiencySulfoneNew classCell cultures
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