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Keywords:

  • click chemistry;
  • drug discovery;
  • multivalency;
  • receptors;
  • steroid hormones
Thumbnail image of graphical abstract

Molecular ruler: Steroid analogues were conjugated to DNA by using click chemistry, and self-assembly provided ternary DNA complexes with bivalent ligand presentation. The distance between the bound ligands was measured by spatial screening of the estrogen receptor, and a second hydrophobic binding site was postulated. The picture shows the DNA(black)–raloxifene(orange) complex in the ligand binding domain of the receptor.