Referenced in: none

Automatically associated channels: TRP , TRPV , TRPV6

Title: Quercetin enhances VDR activity, leading to stimulation of its target gene expression in Caco-2 cells.

Authors: Jun Inoue, Jung-Min Choi, Takehiro Yoshidomi, Takuya Yashiro, Ryuichiro Sato

Journal, date & volume: J. Nutr. Sci. Vitaminol., 2010 , 56, 326-30

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/21228504

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.