Our paper on structure-guided optimization of nanomolar inhibitors of the VHL-HIFalpha protein-protein interaction is now published in J. Med. Chem.

  • ToC graphic
  • Figure 1
  • Figure 2. Crystal structure of VBC in complex with ligand 1 (gray carbons, PDB 3ZRC) and 2 (purple carbons, PDB 4W9C)
  • Figure 3. Crystal structure of VBC in complex with the ligand 7 (orange carbons, PDB 4W9H).
  • Figure 4. Crystal structure of the VBC in complex with (A) ligand 13 (cyan carbons, PDB 4W9J) with bound HIF-1α peptide superposed and (B) ligand 14 (gray carbons, PDB 4W9K).
  • Scheme 1. Synthesis of the Ligand 7.

Read our paper here.