Pregnane X receptor-mediated transcription

被引:9
作者
Chang, TKH [1 ]
Waxman, DJ
机构
[1] Univ British Columbia, Fac Pharmaceut Sci, Vancouver, BC V5Z 1M9, Canada
[2] Boston Univ, Dept Biol, Div Cell & Mol Biol, Boston, MA 02215 USA
来源
PHASE II CONJUGATION ENZYMES AND TRANSPORT SYSTEMS | 2005年 / 400卷
关键词
D O I
10.1016/S0076-6879(05)00033-9
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
The pregnane X receptor (PXR, receptor NR1I2) is a ligand-activated transcription factor that is activated by structurally diverse endogenous steroids and foreign chemicals and serves as an important steroid and xenobiotic sensor. This member of the nuclear receptor superfamily is highly expressed in liver and in the gastrointestinal tract, where it regulates transcription of a large set of genes that contribute to foreign compound metabolism and to the metabolism and transcellular transport of steroid hormones, bile acids, and other endogenous substances. This chapter summarizes studies of PXR and its biological functions and describes a cell culture-based luciferase reporter gene assay for determination of PXR transcriptional activity. This assay can be used to identify novel drugs and environmental chemicals that serve as PXR ligands and thereby modulate PXR activity and may aid in the prediction of drug-drug interactions and foreign chemical-induced toxicities associated with the activation of PXR transcriptional responses.
引用
收藏
页码:588 / 598
页数:11
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