Discovery of small molecules that bind to K-Ras and inhibit Sos-mediated activation.

@article{Sun2012DiscoveryOS,
  title={Discovery of small molecules that bind to K-Ras and inhibit Sos-mediated activation.},
  author={Qi Sun and Jason P Burke and Jason Phan and Michael C Burns and Edward T. Olejniczak and Alex G. Waterson and Taekyu Lee and Olivia W. Rossanese and Stephen W. Fesik},
  journal={Angewandte Chemie},
  year={2012},
  volume={51 25},
  pages={6140-3}
}
K-Ras is a small GTPase that functions as a molecular switch cycling between inactive (guanosine diphosphate [GDP]bound) and active (guanosine triphosphate [GTP]-bound) states. The conversion of K-Ras–GDP to K-Ras–GTP is the rate-limiting step in the activation of K-Ras and is catalyzed by guanine nucleotide exchange factors, such as the son of sevenless (Sos). Mutations in K-Ras fix the protein in the active state and endow cells with capabilities that represent the hallmarks of cancer. These… CONTINUE READING
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