A fluorescence quenching assay to discriminate between specific and nonspecific inhibitors of dengue virus protease
Bodenreider, Christophe; Beer, David; Keller, Thomas H; Sonntag, Sebastian; Wen, Daying; Yap, LiJian; Yau, Yin Hoe; Geifman Shochat, Susana; Huang, Danzhi; Zhou, Ting; Caflisch, Amedeo; Su, Xun-Cheng; Ozawa, Kiyoshi; Vasudevan, Subhash G.; Lescar, Julien; Lim, Siew Pheng; Otting, Gottfried
In drug discovery, the occurrence of false positives is a major hurdle in the search for lead compounds that can be developed into drugs. A small-molecular-weight compound that inhibits dengue virus protease at low micromolar levels was identified in a screening campaign. Binding to the enzyme was confirmed by isothermal titration calorimetry (ITC) and nuclear magnetic resonance (NMR). However, a structure-activity relationship study that ensued did not yield more potent leads. To further...[Show more]
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