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Proteomics-based approach for drug discovery

Liron Bar-Peled, PhD (Damon Runyon Fellow ‘14-‘17) of the Scripps Research Institute, La Jolla, developed a new proteomics-based approach to discover small-molecule inhibitors that could be used as anti-cancer therapies. The approach is based on the fact that certain amino acids on proteins have a special chemical reactivity that allows them to form irreversible covalent bonds with suitably designed probe or "scout" molecules. Scientists can apply such molecules to a large collection of cellular proteins to quickly identify proteins that have these reactive amino-acids -- which would be considered potential drug targets. The researchers applied this strategy to identify potential drug targets in non-small-cell lung cancers (NSCLCs) that depend on over-activity of the transcription factor NRF2. The study was published in the journal Cell.