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Date publication

juillet 2022

Journal

International journal of molecular sciences

Auteurs

Membres identifiés du Cancéropôle Est :
Dr METZGER Daniel , Dr ROCHEL-GUIBERTEAU Natacha , Dr LAVERNY Gilles


Tous les auteurs :
Belorusova AY, Rovito D, Chebaro Y, Doms S, Verlinden L, Verstuyf A, Metzger D, Rochel N, Laverny G

Résumé

The Vitamin D receptor (VDR) plays a key role in calcium homeostasis, as well as in cell proliferation and differentiation. Among the large number of VDR ligands that have been developed, we have previously shown that BXL-62 and Gemini-72, two C-20-modified vitamin D analogs are highly potent VDR agonists. In this study, we show that both VDR ligands restore the transcriptional activities of VDR variants unresponsive to the natural ligand and identified in patients with rickets. The elucidated mechanisms of action underlying the activities of these C-20-modified analogs emphasize the mutual adaptation of the ligand and the VDR ligand-binding pocket.

Mots clés

rare diseases, structure function relationship, vitamin D

Référence

Int J Mol Sci. 2022 07 30;23(15):

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