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Modulators of vitamin D nuclear receptor: recent advances from structural studies

Anna Y Belorusova, Natacha Rochel1

  • 1Department of Integrative Structural Biology, Institut de Genetique et de Biologie Moleculaire et Cellulaire (IGBMC), Institut National de Sante et de Recherche Medicale (INSERM) U964/Centre National de Recherche Scientifique (CNRS) UMR 7104/Universite de Strasbourg, 67404 Illkirch, France. rochel@igbmc.fr.

Current Topics in Medicinal Chemistry
|December 10, 2014
PubMed

Insights

The vitamin D nuclear receptor (VDR) is a therapeutic target for diseases like cancer and autoimmune disorders. Structural analysis of VDR-ligand complexes guides the development of new, selective VDR modulators.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Structural Biology

Background:

  • The vitamin D nuclear receptor (VDR) and its ligand, 1α, 25-dihydroxyvitamin D3 (1,25(OH)2D3), regulate critical biological functions.
  • VDR is a key therapeutic target for diseases including cancers, psoriasis, rickets, renal osteodystrophy, and autoimmune disorders.

Purpose of the Study:

  • To review recent structural data on VDR-ligand complexes.
  • To highlight promising VDR modulators and novel findings in VDR-ligand recognition.

Main Methods:

  • Analysis of crystal structures of VDR-ligand complexes.
  • Review of recently published structural data and scientific literature.

Main Results:

  • Structural information is crucial for explaining and validating VDR modulator properties.
  • Promising compounds include secosteroidal compounds and 1,25(OH)2D3 mimics.
  • Novel VDR modulators and an alternative ligand binding site have been identified.

Conclusions:

  • Continued structural analysis of VDR-ligand interactions is essential for developing selective VDR modulators.
  • The identification of novel ligands and binding sites expands therapeutic potential.

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