Kinetic Studies of Thiosemicarbazone Inhibitors of Cruzain, a Validated Target of Cruzain
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Chagas’ disease is caused by the flagellate protozoan Trypanosoma cruzi. As determined by the World Health Organization, effective therapeutic medications are needed for the treatment of Chagas’ disease. Cruzain, a powerful cysteine protease involved in cell invasion, immune evasion, and metabolism of the T. cruzi parasite, is a validated target for the disease. A number of thiosemicarbazone derivatives are inhibitors of cruzain. In this study, the kinetic mechanism of a potent thiosemicarbazone inhibitor of cruzain was investigated. A microplate reader using a 96-well plate format was used to perform fluorometric assays. Progress curves provided evidence that this thiosemicarbazone compound is a time-dependent inhibitor of cruzain. This was a collaborative study between the Trawick and Pinney groups at Baylor University.