Activity-based proteomics: enzyme chemistry redux

The principles of enzyme chemistry, mechanism of action and inhibitor design are being applied to proteomics by the development of activity-based probes. This approach suggests a potentially broad method for interrogating enzyme family members, both known and unknown, in cells and proteomic fractions without the need for individual assay development and isolation. The serine hydrolases and cysteine proteases have provided the proofs of concept for activity-based proteomics, and other studies are rapidly following. The result will be a proteomics technology of great value to drug discovery and development.