Journal
NATURE CHEMICAL BIOLOGY
Volume 5, Issue 6, Pages 394-396Publisher
NATURE PUBLISHING GROUP
DOI: 10.1038/nchembio.162
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Funding
- German Federal Ministry for Education and Research through the German National Genome Research Network-Plus (NGFN-Plus) [BMBF 01GS08102]
- Schering Plough
- Bayer-Schering Pharma
- Merck-Serono
- Bayer CropScience
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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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