Target identification of covalently binding drugs by activity-based protein profiling (ABPP)

Abstract

The characterization of the target proteins of drug molecules has become an important goal in understanding its mode of action and origin of side effects due to off-target binding. This is especially important for covalently binding drugs usually containing electrophilic moieties, which potentially can react with nucleophilic residues found in many proteins. This review gives a comprehensive overview of the use of activity-based protein profiling (ABPP) as an efficient tool for the target identification of covalently binding drugs.

Keywords: Activity based protein profiling; Biologically active molecules; Covalent binding drugs; Drug targets; Target identification.