Most drug targets are cellular proteins that selectively interact with chemicals administered to treat
diseases. Chemical proteomics, as an interdisciplinary technology that integrates synthetic and analytic
chemistry, biochemistry and cell biology, has recently emerged as a powerful platform to specifically enrich and
comprehensively profile drug-binding proteins, and thus has been extensively applied in the identification of
drug targets. In addition, chemical proteomics can also provide information for researchers to understand the
poly-pharmacological activities of the pharmaceutical compounds, and thus help in maximizing the efficacy and
minimizing the side effects of the drugs. In this manuscript, we summarized several popular approaches of
chemical proteomics by illustrating their essential features in drug target-fishing through specific profiling of
drug-protein interaction. Alternative technologies for target identification were also discussed.
Keywords: Affinity chromatography, chemical proteomics, mass spectrometry, photoaffinity labeling strategies,
quantitative proteomics, target fishing.
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