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DNA-Controlled Bivalent Presentation of Ligands for the Estrogen Receptor

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  • This work was supported by the Deutsche Forschungsgemeinschaft (SFB 765).

Abstract

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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.

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