Downsizing the BAD BH3 peptide to small constrained α-helices with improved ligand efficiency.

@article{Shepherd2016DownsizingTB,
  title={Downsizing the BAD BH3 peptide to small constrained α-helices with improved ligand efficiency.},
  author={Nicholas E. Shepherd and Rosemary S. Harrison and Gloria Ruiz-G{\'o}mez and Giovanni Abbenante and Jody M Mason and David P. Fairlie},
  journal={Organic & biomolecular chemistry},
  year={2016},
  volume={14 46},
  pages={10939-10945}
}
Bcl2 Homology (BH) proteins can either trigger or prevent programmed cell death or apoptosis. Deregulation of the BH protein family network leads to evasion of apoptosis, uncontrolled proliferation and is a hallmark of cancer. Inhibition of pro-survival BH proteins is a promising chemotherapeutic strategy for certain cancers. We have examined whether helix-constrained peptides based on the BAD BH3 domain (residues 103-127) can be downsized to much smaller more drug-like peptides. We report the… CONTINUE READING