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Nat Chem Biol. 2009 Jun;5(6):394-6. doi: 10.1038/nchembio.162. Epub 2009 Apr 26.

A new screening assay for allosteric inhibitors of cSrc.

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  • 1Chemical Genomics Centre of the Max Planck Society, Dortmund, Germany.


Targeting kinases outside the highly conserved ATP pocket is thought to be a promising strategy for overcoming bottlenecks in kinase inhibitor research, such as limited selectivity and drug resistance. Here we report the development and application of a direct binding assay to detect small molecules that stabilize the inactive conformation of the tyrosine kinase cSrc. Protein X-ray crystallography validated the assay results and confirmed an exclusively allosteric binding mode.

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