Abstract
Developing selective and potent drugs for a protein target to treat human disease is an extremely challenging endeavor. Successful drug discovery relies heavily on thorough and unbiased therapeutic target validation and understanding the mechanism of action of the drug candidates. In general, phenotypic screening in disease-relevant models identifies small molecule hits with desirable efficacy but often with unknown modes of action. Probe-based chemical proteomics technologies have been shown to play an integral role in target identification and validation of the biological target(s) through which the drug is proposed to exert its mechanistic effects. This chapter discusses the utilization of chemical probes for target identification, target deconvolution, and target engagement studies. The Chapter is divided into two parts: the first part covers covalent activity-based and reactivity-based probes, mainly cysteine and lysine targeting chemical probes, and the second part covers noncovalent photoaffinity probes.
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