In Vivo Activation of the p53 Pathway by Small-Molecule Antagonists of MDM2

@article{Vassilev2004InVA,
  title={In Vivo Activation of the p53 Pathway by Small-Molecule Antagonists of MDM2},
  author={Lyubomir T Vassilev and Binh Thanh Vu and Bradford J. Graves and Daisy M. Carvajal and Frank Podlaski and Zoran M Filipovic and Norman Kong and Ursula Kammlott and Christine M. Lukacs and Christian L Klein and Nader Fotouhi and Emily Aijun Burlingame Liu},
  journal={Science},
  year={2004},
  volume={303},
  pages={844 - 848}
}
MDM2 binds the p53 tumor suppressor protein with high affinity and negatively modulates its transcriptional activity and stability. Overexpression of MDM2, found in many human tumors, effectively impairs p53 function. Inhibition of MDM2-p53 interaction can stabilize p53 and may offer a novel strategy for cancer therapy. Here, we identify potent and selective small-molecule antagonists of MDM2 and confirm their mode of action through the crystal structures of complexes. These compounds bind MDM2… 
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