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Keywords:

  • combinatorial chemistry;
  • fragment-based screening;
  • microarrays;
  • protein–protein interactions;
  • proteins
Thumbnail image of graphical abstract

The way to a 14-3-3 binder: A fragment-based combinatorial small-molecule microarray generates affinity-based fingerprints of the 14-3-3σ protein. One small molecule (see picture; in red box) that disrupts the 14-3-3/protein interaction (green/blue) has been identified. The compound is cell-permeable and possesses both in vitro and in-cell activities.