Characterization of Drug–Protein Interactions by Chemoproteomics

Chemoproteomics can be defined as the study of protein–bioactive molecule interactions on a proteome‐wide scale. This branch of proteomics has become an important tool in drug discovery as well as basic biomedical research as it allows the definition of the protein “interactome” of small molecules and drugs as a means for target identification, target deconvolution, and elucidation of the mechanism of action (MoA) of drug candidates as well as the investigation of cellular processes such as the regulation of signaling pathways and enzymatic activities. In this chapter, a number of experimental concepts and strategies as well as areas of application of chemoproteomics are discussed in the context of selected literature examples.