Discovery of a Potent and Selective DDR1 Receptor Tyrosine Kinase Inhibitor

@inproceedings{Kim2013DiscoveryOA,
  title={Discovery of a Potent and Selective DDR1 Receptor
Tyrosine Kinase Inhibitor},
  author={Hyung-Gu Kim and Li Tan and Ellen Weisberg and Feiyang Liu and Peter Connor Canning and Hwan Geun Choi and Scott A. Ezell and Hong Wu and Zheng Nan Zhao and Jinhua Wang and Anna Mandinova and James D Griffin and Alex N Bullock and Qingsong Liu and Sam W. Lee and Nathanael S Gray},
  booktitle={ACS chemical biology},
  year={2013}
}
The DDR1 receptor tyrosine kinase is activated by matrix collagens and has been implicated in numerous cellular functions such as proliferation, differentiation, adhesion, migration, and invasion. Here we report the discovery of a potent and selective DDR1 inhibitor, DDR1-IN-1, and present the 2.2 Å DDR1 co-crystal structure. DDR1-IN-1 binds to DDR1 in the 'DFG-out' conformation and inhibits DDR1 autophosphorylation in cells at submicromolar concentrations with good selectivity as assessed… CONTINUE READING
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