Small molecule RITA binds to p53, blocks p53–HDM-2 interaction and activates p53 function in tumors

@article{Issaeva2004SmallMR,
  title={Small molecule RITA binds to p53, blocks p53–HDM-2 interaction and activates p53 function in tumors},
  author={Natalia Issaeva and Przemyslaw Bozko and Martin Enge and Marina Nikolaevna Protopopova and Lisette G G C Verhoef and Maria G Masucci and Aladdin Pramanik and Galina A. Selivanova},
  journal={Nature Medicine},
  year={2004},
  volume={10},
  pages={1321-1328}
}
In tumors that retain wild-type p53, its tumor-suppressor function is often impaired as a result of the deregulation of HDM-2, which binds to p53 and targets it for proteasomal degradation. We have screened a chemical library and identified a small molecule named RITA (reactivation of p53 and induction of tumor cell apoptosis), which bound to p53 and induced its accumulation in tumor cells. RITA prevented p53–HDM-2 interaction in vitro and in vivo and affected p53 interaction with several… CONTINUE READING
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