title: Quercetin enhances VDR activity, leading to stimulation of its target gene expression in Caco-2 cells.
abstract: Vitamin 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.
authors.affiliation: Department of Applied Biological Chemistry, Graduate School of Agricultural and Life Sciences, The University of Tokyo, Japan.
authors.forename: Jun
authors.initials: J
authors.lastname: Inoue
authors.forename: Jung-Min
authors.initials: JM
authors.lastname: Choi
authors.forename: Takehiro
authors.initials: T
authors.lastname: Yoshidomi
authors.forename: Takuya
authors.initials: T
authors.lastname: Yashiro
authors.forename: Ryuichiro
authors.initials: R
authors.lastname: Sato
mesh_terms: D018938:Caco-2 Cells; D015220:Calcium Channels / Q000235:genetics; D005786:Gene Expression Regulation; D057809:HEK293 Cells; D006801:Humans; D008024:Ligands; D011794:Quercetin / Q000378:metabolism*; D018167:Receptors, Calcitriol / Q000235:genetics* / Q000378:metabolism*; D050916:TRPV Cation Channels / Q000235:genetics; D015533:Transcriptional Activation
chemical_list: D015220:Calcium Channels; D008024:Ligands; D018167:Receptors, Calcitriol; D050916:TRPV Cation Channels; C422827:TRPV6 protein, human; D011794:Quercetin