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Coordinate transcriptional regulation of transport and metabolism

Eloranta, Jyrki J. and Meier, Peter J. and Kullak-Ublick, Gerd A.. (2005) Coordinate transcriptional regulation of transport and metabolism. Methods in enzymology, vol. 400. S. 511-530.

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Official URL: http://edoc.unibas.ch/dok/A5261583

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Abstract

Intestinal absorption and hepatic clearance of drugs, xenobiotics, and bile acids are mediated by transporter proteins expressed at the plasma membranes of intestinal epithelial cells and liver parenchymal cells in a polarized manner. Within enterocytes and hepatocytes, these exogenous or endogenous, potentially toxic compounds may be metabolized by phase I cytochrome P450 (CYP) and phase II conjugating enzymes. Many transporter proteins and metabolizing enzymes are subject to direct translational modification, enabling very rapid changes in their activity. However, to achieve intermediate and longer term changes in transport and enzyme activities, the genes encoding drug and bile acid transporters, as well as the CYP and conjugating enzymes, are regulated by a complex network of transcriptional cascades. These are typically mediated by specific members of the nuclear receptor family of transcription factors, particularly FXR, SHP, PXR, CAR, and HNF-4alpha. Most nuclear receptors are activated by specific ligands, including numerous xenobiotics (PXR, CAR) and bile acids (FXR). The fine-tuning of transcriptional control of drug and bile acid homeostasis depends on regulated interactions of specific nuclear receptors with their target genes.
Faculties and Departments:11 Rektorat und Verwaltung > Vizerektorat Forschung
UniBasel Contributors:Meier-Abt, Peter J.
Item Type:Article, refereed
Bibsysno:Link to catalogue
Note:Also published in: Phase II conjugation enzymes and transport systems. - Amsterdam : Elsevier, 2005. - S. 511-530 -- Publication type according to Uni Basel Research Database: Journal article
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Last Modified:22 Mar 2012 14:27
Deposited On:22 Mar 2012 13:59

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