Kathleen E Rogers, Henrik Keränen, Jacob D. Durrant, Joseline Ratnam, Allison Doak, Michelle R. Arkin and J. Andrew McCammon Novel Cruzain Inhibitors for the Treatment of Chagas’ Disease Chemical Biology & Drug Design 80
Article first published online: 27 JUN 2012 | DOI: 10.1111/j.1747-0285.2012.01416.x
Trypanosoma cruzi, the etiological agent of Chagas’ disease, affects millions of individuals and current therapies are inadequate. Using an exhaustive virtual-screening and experimental-validation approach, we identify several small-molecule inhibitors of cruzain, an essential cysteine protease of the protozoan parasite T. cruzi. Optimization of these chemical scaffolds could lead to the development of direly needed novel drugs useful in the treatment of Chagas’ disease.
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