Article
A vitamin D receptor selectively activated by gemini analogs reveals ligand dependent and independent effects.
Cell reports - 3 Feb 2015
Huet Tiphaine, Laverny Gilles, Ciesielski Fabrice, Molnár Ferdinand, Ramamoorthy Thanuja Gali, Belorusova Anna Y, Antony Pierre, Potier Noelle, Metzger Daniel, Moras Dino, Rochel Natacha
Abstract excerpt
The bioactive form of vitamin D [1,25(OH)2D3] regulates mineral and bone homeostasis and exerts potent anti-inflammatory and antiproliferative properties through binding to the vitamin D receptor (VDR). The 3D structures of the VDR ligand-binding domain with 1,25(OH)2D3 or gemini analogs unveiled the molecular mechanism underlying ligand recognition. On the basis of structure-function correlations, we generated a...
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