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lüll Quercetin enhances VDR activity, leading to stimulation of its target gene expression in Caco-2 cells Inoue J; Choi JM; Yoshidomi T; Yashiro T; Sato RJ Nutr Sci Vitaminol (Tokyo) 2010[]; 56 (5): 326-30Vitamin D receptor (VDR) is a nuclear receptor that regulates the expression of genes involved in calcium homeostasis. Activation of VDR is thought to be a promising drug target for osteoporosis. Using a VDR-driven luciferase expression assay for screening a naturally occurring food component, we identified quercetin as a VDR activator. Quercetin also activated the GAL4 DNA-binding domain fused to the VDR ligand-binding domain. Moreover, it was confirmed that quercetin increases the mRNA level of TRPV6, which is a VDR target gene, in Caco-2 cells. These results indicate that quercetin enhances VDR activity through the alteration of cofactor recruitment, thereby stimulating its target genes while providing a new function for quercetin as the VDR activator.|*Gene Expression Regulation[MESH]|Caco-2 Cells[MESH]|Calcium Channels/genetics[MESH]|HEK293 Cells[MESH]|Humans[MESH]|Ligands[MESH]|Quercetin/*metabolism[MESH]|Receptors, Calcitriol/*genetics/*metabolism[MESH]|TRPV Cation Channels/genetics[MESH]|Transcriptional Activation[MESH] |