New directions in targeting protein kinases: focusing upon true allosteric and bivalent inhibitors.

@article{Lamba2012NewDI,
  title={New directions in targeting protein kinases: focusing upon true allosteric and bivalent inhibitors.},
  author={Vandana Lamba and Indraneel Ghosh},
  journal={Current pharmaceutical design},
  year={2012},
  volume={18 20},
  pages={
          2936-45
        }
}
Over the past decade, therapeutics that target subsets of the 518 human protein kinases have played a vital role in the fight against cancer. Protein kinases are typically targeted at the adenosine triphosphate (ATP) binding cleft by type I and II inhibitors, however, the high sequence and structural homology shared by protein kinases, especially at the ATP binding site, inherently leads to polypharmacology. In order to discover or design truly selective protein kinase inhibitors as both… CONTINUE READING

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