Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
6291887 | Experimental Parasitology | 2011 | 6 Pages |
Abstract
⺠The trypanocidial bioflavanoid quercetin (QCN) is a potent mixed inhibitor of Trypanosoma brucei hexokinase 1 (TbHK1) (IC50 = 4.1 ± 0.8 μM). ⺠QCN binds close to the enzyme active site and influences fluorescence of the single tryptophan residue, much like ATP does. ⺠In live parasites, QCN localizes in part to glycosomes, the subcellular organelle that houses TbHK1. ⺠T. brucei that over-express TbHK1 are more resistant to QCN, while cells with reduced TbHK1 are more sensitive, suggesting that TbHK1 is a target of the compound.
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Authors
Heidi C. Dodson, Todd A. Lyda, Jeremy W. Chambers, Meredith T. Morris, Kenneth A. Christensen, James C. Morris,