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Cruzipains as a target for Chagas disease: inhibitor discovery and characterization of subtypes

Abstract: Due to the low efficacy and serious side effects of the currently available pharmacotherapy for Chagas disease, there is a need to develop effective and selective drugs against this protozoan. Among the targets studied, cruzipains are a multigene family of cysteine ??proteases with important roles in the parasite life cycle. In this presentation, we will describe recent studies from our lab that led to the discovery and characterization of cruzain inhibitors with trypanocidal activity. In addition, we will discuss our studies that allowed the classification of cruzipains into four subtypes. Molecular modeling studies indicate significant differences in the active sites of these subtypes, with a potential impact on T. cruzi biology and inhibitor discovery. 

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BrazMedChem