Development of a potent Bcl-x(L) antagonist based on alpha-helix mimicry.

  title={Development of a potent Bcl-x(L) antagonist based on alpha-helix mimicry.},
  author={Olaf Kutzki and Hyung Soon Park and Justin T. Ernst and Brendan P Orner and Hang Yin and Andrew D. Hamilton},
  journal={Journal of the American Chemical Society},
  volume={124 40},
The rational design of low-molecular weight ligands that disrupt protein-protein interactions is still a challenging goal in medicinal chemistry. Our approach to this problem involves the design of molecular scaffolds that mimic the surface functionality projected along one face of an alpha-helix. Using a terphenyl scaffold, which in a staggered conformation closely reproduces the projection of functionality on the surface of an alpha-helix, we designed mimics of the pro-apoptotic alpha-helical… CONTINUE READING
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