Article
Structural insights into the molecular mechanism of vitamin D receptor activation by lithocholic acid involving a new mode of ligand recognition.
Journal of medicinal chemistry - 12 Jun 2014
Belorusova Anna Y, Eberhardt Jérôme, Potier Noëlle, Stote Roland H, Dejaegere Annick, Rochel Natacha
Abstract excerpt
The vitamin D receptor (VDR), an endocrine nuclear receptor for 1α,25-dihydroxyvitamin D3, acts also as a bile acid sensor by binding lithocholic acid (LCA). The crystal structure of the zebrafish VDR ligand binding domain in complex with LCA and the SRC-2 coactivator peptide reveals the binding of two LCA molecules by VDR. One LCA binds to the canonical ligand-binding pocket, and the second one, which is not...
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