Quantification of the Vitamin D Receptor-Coregulator Interaction

    January 2009 in “ Biochemistry ”
    Arnaud Teichert, Leggy A. Arnold, Steve Otieno, Yuko Oda, Indre Augustinaite, Tim Geistlinger, Richard W. Kriwacki, R. Kiplin Guy, Daniel D. Bikle
    TLDR Vitamin D receptor binds similarly to natural and synthetic ligands, affecting gene regulation.
    The study evaluated the interaction between the vitamin D receptor (VDR) and various coregulator binding motifs using two ligands: the natural ligand 1α,25(OH)2D3 and a synthetic agonist LG190178. It was found that VDR had a high affinity for specific LxxLL motifs in SRC1, SRC2, SRC3, and DRIP205, with similar binding patterns for both ligands, suggesting similar biological functions. The corepressor Hairless (Hr) bound VDR through a LxxLL motif, repressing transcription regardless of ligand presence. These findings could help predict tissue-specific VDR functions and aid in developing targeted vitamin D response modulators.
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