PLoS neglected tropical diseases · 2010 · 103 citations · 32 references
We demonstrate that WRR-483 is an effective cysteine protease inhibitor with trypanocidal activity in cell culture and animal model with comparable efficacy to K11777. Crystallographic evidence confirms that the mode of action is by targeting the active site of cruzain. Taken together, these results suggest that WRR-483 has potential to be developed as a treatment for Chagas' disease.
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Vinyl Sulfones as Antiparasitic Agents and a Structural Basis for Drug Design
Iain D. Kerr, Ji Hae Lee, Christopher J. Farady et al. · Journal of Biological Chemistry · 2009 · 291 citations · Full text