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Trends Biotechnol. 2018 Dec;36(12):1275-1286. doi: 10.1016/j.tibtech.2018.06.008. Epub 2018 Jul 13.

Chemoproteomics and Chemical Probes for Target Discovery.

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Cellzome GmbH, a GSK Company, Meyerhofstrasse 1, D-69117 Heidelberg, Germany. Electronic address:
Institute for Pharmaceutical Chemistry, Johann Wolfgang Goethe-University, D-60438 Frankfurt am Main, Germany; Buchmann Institute for Molecular Life Sciences, Structural Genomics Consortium, Johann Wolfgang Goethe-University, D-60438 Frankfurt am Main, Germany; German Cancer Consortium DKTK, Frankfurt/Mainz, Germany; Electronic address:


Chemical probes represent versatile tools to validate disease-modifying targets. However, evaluating the selectivity of chemical probes in complex cellular systems is a major challenge that needs to be addressed to better understand the mode of action of small molecules and the interpretation of their pharmacological effects. Chemoproteomics has emerged as a key technology to characterize the mode of action of pharmacological modulators such as chemical probes and drugs, and these studies have unraveled the cellular targets of many bioactive compounds. Here we review the role of chemical probes for the validation of new therapeutic targets and their characterization by proteome wide affinity- and activity-based chemical proteomics and recently developed label-free technologies.


chemical probes; chemical proteomics; drug discovery; mass spectrometry; target validation

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