Afficher la couverture 'Vitamin D Analogs Bearing C-20 Modifications Stabilize the Agonistic Conformation of Non-Responsive Vitamin D Receptor Variants | Belorusova, Anna' en grand format
/5

0 avis

Vitamin D Analogs Bearing C-20 Modifications Stabilize the Agonistic Conformation of Non-Responsive Vitamin D Receptor Variants

Archive ouverte

Belorusova, Anna | Rovito, Daniela | Chebaro, Yassmine | Doms, Stefanie | Verlinden, Lieve | Verstuyf, Annemieke | Metzger, Daniel | Rochel, Natacha | Laverny, Gilles

Edité par CCSD ; MDPI -

International audience. 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.

Suggestions

Du même auteur

Structural analysis and biological activities of C25-amino and C25-nitro vitamin D analogs

Archive ouverte | Gómez-Bouzó, Uxía | CCSD

International audience. Intense synthetic efforts have been directed towards the development of noncalcemic analogs of 1,25-dihydroxyvitamin D 3. We describe here the structural analysis and biological evaluation of...

Cytosolic sequestration of the vitamin D receptor as a therapeutic option for vitamin D-induced hypercalcemia

Archive ouverte | Rovito, Daniela | CCSD

International audience. The bioactive vitamin D3, 1α,25(OH)2D3, plays a central role in calcium homeostasis by controlling the activity of the vitamin D receptor (VDR) in various tissues. Hypercalcemia secondary to ...

A vitamin D‐based strategy overcomes chemoresistance in prostate cancer

Archive ouverte | Len‐tayon, Kateryna | CCSD

International audience. Background and purpose Castration‐resistant prostate cancer (CRPC) is a common male malignancy that requires new therapeutic strategies due to acquired resistance to its first‐line treatment,...

Chargement des enrichissements...