Chemical Proteomics to Identify Molecular Targets of Small Compounds

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.