Activity-based Protein Profiling

Genome sequencing projects have revolutionized our view of the complexity of prokaryotic and eukaryotic proteomes, however, we are also left with a daunting challenge of functionally annotating these large number of predicted proteins. Activity-based protein profiling (ABPP) has been developed as a powerful chemoproteomic tool aiming at systematically discovering and assigning functions of uncharacterized enzymes directly from native proteomes. Here, we reviewed the development and application of this emerging technique, mainly focusing on how it was applied for functional annotation of unknown enzymes, screening and optimization of small-molecule inhibitors, and target identification of bio-active small molecules.