Well done to Greg Craven on his first author paper in Angew. Chem. Int. Ed.!
The paper, ‘High-Throughput Kinetic Analysis for Target-Directed Covalent Ligand Discovery’, reports quantitative irreversible tethering (qIT) as a general technique for screening cysteine-reactive small molecules. The method enables screening of electrophilic fragments with different reactivity by parallel kinetic analysis of target and control thiols. qIT was then applied to the protein Cdk2 and used to identify a covalent inhibitor with a new mode-of-action.
Congratulations to all those involved in the project!
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Charlotte Sutherell
Department of Chemistry
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Tel: +44 (0)20 7594 8141
Email: c.sutherell@imperial.ac.uk
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