Non-ATP competitive protein kinase inhibitors.

  title={Non-ATP competitive protein kinase inhibitors.},
  author={Laura Garuti and Marinella Roberti and Giovanni Bottegoni},
  journal={Current medicinal chemistry},
  volume={17 25},
Protein kinases represent an attractive target in oncology drug discovery. Most of kinase inhibitors are ATP-competitive and are called type I inhibitors. The ATP-binding pocket is highly conserved among members of the kinase family and it is difficult to find selective agents. Moreover, the ATP-competitive inhibitors must compete with high intracellular ATP levels leading to a discrepancy between IC50s measured by biochemical versus cellular assays. The non-ATP competitive inhibitors, called… CONTINUE READING
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