Ordering of the N-terminus of human MDM2 by small molecule inhibitors.

@article{Michelsen2012OrderingOT,
  title={Ordering of the N-terminus of human MDM2 by small molecule inhibitors.},
  author={Klaus Michelsen and John Brad Jordan and Jeffrey Lewis and Alexander Makenzie Long and Evelyn Y Yang and Yosup Rew and Jing Zhou and Peter S. Yakowec and Paul Schnier and Xingzhen Huang and Leszek Poppe},
  journal={Journal of the American Chemical Society},
  year={2012},
  volume={134 41},
  pages={
          17059-67
        }
}
Restoration of p53 function through the disruption of the MDM2-p53 protein complex is a promising strategy for the treatment of various types of cancer. Here, we present kinetic, thermodynamic, and structural rationale for the remarkable potency of a new class of MDM2 inhibitors, the piperidinones. While these compounds bind to the same site as previously reported for small molecule inhibitors, such as the Nutlins, data presented here demonstrate that the piperidinones also engage the N… CONTINUE READING
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