PT  - JOURNAL ARTICLE
AU  - Zhimin Ou
AU  - Mengxi Jiang
AU  - Bingfang Hu
AU  - Yixian Huang
AU  - Meishu Xu
AU  - Songrong Ren
AU  - Song Li
AU  - Suhuan Liu
AU  - Wen Xie
AU  - Min Huang
TI  - Transcriptional Regulation of Human Hydroxysteroid Sulfotransferase SULT2A1 by LXR<em>α</em>
AID  - 10.1124/dmd.114.058479
DP  - 2014 Oct 01
TA  - Drug Metabolism and Disposition
PG  - 1684--1689
VI  - 42
IP  - 10
4099  - http://dmd.aspetjournals.org/content/42/10/1684.short
4100  - http://dmd.aspetjournals.org/content/42/10/1684.full
SO  - Drug Metab Dispos2014 Oct 01; 42
AB  - The nuclear receptor liver X receptor (LXR) plays an important role in the metabolism and homeostasis of cholesterol, lipids, bile acids, and steroid hormones. In this study, we uncovered a function of LXRα (NR1H3) in regulating the human hydroxysteroid sulfotransferase SULT2A1, a phase II conjugating enzyme known to sulfonate bile acids, hydroxysteroid dehydroepiandrosterone, and related androgens. We showed that activation of LXR induced the expression of SULT2A1 at mRNA, protein, and enzymatic levels. A combination of promoter reporter gene and chromatin immunoprecipitation assays showed that LXRα transactivated the SULT2A1 gene promoter through its specific binding to the −500- to −258-base pair region of the SULT2A1 gene promoter. LXR small interfering RNA knockdown experiments suggested that LXRα, but not LXRβ, played a dominant role in regulating SULT2A1. In primary human hepatocytes, we found a positive correlation between the expression of SULT2A1 and LXRα, which further supported the regulation of SULT2A1 by LXRα. In summary, our results established human SULT2A1 as a novel LXRα target gene. The expression of LXRα is a potential predictor for the expression of SULT2A1 in human liver.