Structure-based discovery of the first allosteric inhibitors of cyclin-dependent kinase 2.

@article{Rastelli2014StructurebasedDO,
  title={Structure-based discovery of the first allosteric inhibitors of cyclin-dependent kinase 2.},
  author={Giulio Rastelli and Andrew Anighoro and Martina Chripkova and Laura Carrassa and Massimo Broggini},
  journal={Cell cycle},
  year={2014},
  volume={13 14},
  pages={
          2296-305
        }
}
Allosteric targeting of protein kinases via displacement of the structural αC helix with type III allosteric inhibitors is currently gaining a foothold in drug discovery. Recently, the first crystal structure of CDK2 with an open allosteric pocket adjacent to the αC helix has been described, prospecting new opportunities to design more selective inhibitors, but the structure has not yet been exploited for the structure-based design of type III allosteric inhibitors. In this work we report the… CONTINUE READING

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