Activity‐Based Protein Profiling

Activity-based protein profiling (ABPP) is a powerful and versatile chemical proteomic platform that can be used for a wide range of biological applications, including protein characterization and drug discovery. ABPP uses activity-based probes (ABPs) that are chemical tools based on small molecule inhibitors. These probes can interrogate the inhibitor's protein interaction profile and quantify associated enzyme activities in living systems. Identification of a molecule's target proteins can provide vital information for drug development, as well as revealing mode(s) of action and structure–activity relationship data. In this chapter, we present the fundamentals of ABPP strategy, including ABP design and quantitative proteomic approaches for robust protein profiling. In addition, we describe how ABPP has been used in recent biological studies, highlighting key applications that relate to drug discovery and development.