Nuclear-receptor–mediated regulation of drug– and bile-acid–transporter proteins in gut and liver
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Issue Date
2013-02Author
Staudinger, Jeffrey Leonard
Woody, Sarah K.
Sun, Mengxi
Cui, Wenqi
Publisher
Taylor & Francis
Type
Article
Article Version
Scholarly/refereed, author accepted manuscript
Metadata
Show full item recordAbstract
Adverse drug events (ADEs) are a common cause of patient morbidity and mortality and are classically thought to result, in part, from variation in expression and activity of hepatic enzymes of drug metabolism. It is now known that alterations in the expression of genes that encode drug- and bile-acid–transporter proteins in both the gut and liver play a previously unrecognized role in determining patient drug response and eventual clinical outcome. Four nuclear receptor (NR) superfamily members, including pregnane X receptor (PXR, NR1I2), constitutive androstane receptor (NR1I3), farnesoid X receptor (NR1H4), and vitamin D receptor (NR1I1), play pivotal roles in drug- and bile-acid– activated programs of gene expression to coordinately regulate drug- and bile-acid transport activity in the intestine and liver. This review focuses on the NR-mediated gene activation of drug and bile-acid transporters in these tissues as well as the possible underlying molecular mechanisms.
Description
This is an Accepted Manuscript of an article published by Taylor & Francis in Drug Metabolism Reviews on 2015 Sep 2, available online: http://www.tandfonline.com/10.3109/03602532.2012.748793.
Collections
- Pharmacy Scholarly Works [293]
Citation
Staudinger, J. L., Woody, S., Sun, M., & Cui, W. (2013). Nuclear-receptor–mediated regulation of drug– and bile-acid–transporter proteins in gut and liver. Drug Metabolism Reviews, 45(1), 48–59. http://doi.org/10.3109/03602532.2012.748793
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