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Drug Discov Today. 2009 Feb;14(3-4):178-84. doi: 10.1016/j.drudis.2008.09.014. Epub 2008 Nov 18.

Seeing small molecules in action with bioorthogonal chemistry.

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  • 1The Laboratory of Chemical Biology and Microbial Pathogenesis, The Rockefeller University, 1230 York Avenue Box 250, New York, NY 10065, United States.


Chemical probes that target specific protein families offer powerful tools to accelerate drug discovery. Small molecules modified with uniquely reactive functional groups and detection tags provide novel tools to characterize complex proteomes functionally and also to help determine the specificity of small molecule inhibitors toward various enzyme/protein classes. This review highlights the application of bioorthogonal chemistries in combination with chemical probes, which together are offering unprecedented opportunities to dissect the functions of enzyme/protein families in vivo and enabling more precise target identification of small molecules. Advances in chemical probes and bioorthogonal reactions are poised to reveal new therapeutic targets and to facilitate the discovery and characterization of small molecules aimed at disease.

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