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Structure-based design of a superagonist ligand for the vitamin D nuclear receptor.

Archive ouverte | Hourai, Shinji | CCSD

Vitamin D nuclear receptor (VDR), a ligand-dependent transcriptional regulator, is an important target for multiple clinical applications, such as osteoporosis and cancer. Since exacerbated increase of calcium serum level is curre...

Design, Synthesis, Evaluation, and Structure of Vitamin D Analogues with Furan Side Chains

Archive ouverte | Fraga, Ramón | CCSD

International audience. Abstract Based on the crystal structures of human vitamin D receptor (hVDR) bound to 1α,25-dihydroxy-vitamin D 3 (1,25 D) and superagonist ligands, we previously designed new superagonist lig...

The "Phantom Effect" of the Rexinoid LG100754: structural and functional insights.

Archive ouverte | Sato, Yoshiteru | CCSD

International audience. Retinoic acid receptors (RARs) and Retinoid X nuclear receptors (RXRs) are ligand-dependent transcriptional modulators that execute their biological action through the generation of functiona...

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