Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design

@article{Ostrem2016DirectSI,
  title={Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design},
  author={Jonathan M. L. Ostrem and Kevan M. Shokat},
  journal={Nature Reviews Drug Discovery},
  year={2016},
  volume={15},
  pages={771-785}
}
KRAS is the most frequently mutated oncogene in human cancer. In addition to holding this distinction, unsuccessful attempts to target this protein have led to the characterization of RAS as 'undruggable'. However, recent advances in technology and novel approaches to drug discovery have renewed hope that a direct KRAS inhibitor may be on the horizon. In… CONTINUE READING