Direct inhibition of the NOTCH transcription factor complex

@article{Moellering2009DirectIO,
  title={Direct inhibition of the NOTCH transcription factor complex},
  author={Raymond E Moellering and Melanie Cornejo and Tina N. Davis and Cristina Del Bianco and Jon C Aster and Stephen C Blacklow and Andrew L Kung and Dwight Gary Gilliland and Gregory L. Verdine and James E. Bradner},
  journal={Nature},
  year={2009},
  volume={462},
  pages={182-188}
}
Direct inhibition of transcription factor complexes remains a central challenge in the discipline of ligand discovery. In general, these proteins lack surface involutions suitable for high-affinity binding by small molecules. Here we report the design of synthetic, cell-permeable, stabilized α-helical peptides that target a critical protein–protein interface in the NOTCH transactivation complex. We demonstrate that direct, high-affinity binding of the hydrocarbon-stapled peptide SAHM1 prevents… CONTINUE READING
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