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Keywords:

  • antagonists;
  • drug discovery;
  • multicomponent reactions;
  • p53/Hdm2 interaction;
  • protein–protein interactions
Thumbnail image of graphical abstract

The parallel discovery of multiple scaffolds useful to antagonize the cancer-relevant protein–protein interaction p53/Hdm2 is described. The new method is based on the tightly interwoven interplay of multicomponent reaction chemistry, structural biology, computational chemistry, and high-content NMR-based screening.