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Updated: May 25, 2026

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
Published on: December 1, 2020
How chemoproteomics can enable drug discovery and development
Raymond E Moellering1, Benjamin F Cravatt
1The Skaggs Institute for Chemical Biology and Department of Chemical Physiology, The Scripps Research Institute, La Jolla, CA 92037, USA.
Integrating chemical proteomic platforms early in drug discovery can identify new therapeutic targets. This approach expands the range of pharmacologically evaluated proteins, aiding the development of first-in-class medications for human diseases.
Area of Science:
- Pharmacology
- Proteomics
- Drug Discovery
Background:
- Developing novel medications for human diseases is complex.
- Genetics increasingly links mutations to disorders, but pharmacology is key for target validation.
Purpose of the Study:
- To discuss the integration of chemical proteomic platforms in early drug discovery.
- To highlight the potential of these platforms in identifying and prioritizing new therapeutic targets.
Main Methods:
- Utilizing chemical proteomic platforms, such as activity-based protein profiling.
- Applying these platforms in the initial stages of the drug discovery pipeline.
Main Results:
- Expanded scope of proteins pharmacologically evaluated in living systems.
- Facilitated identification and prioritization of novel therapeutic targets.
Conclusions:
- Chemical proteomics offers a powerful approach to advance drug discovery.
- This integration can accelerate the development of first-in-class therapeutics by enabling broader target evaluation.
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