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This version published online on June 16, 2005
Molecular Endocrinology, doi:10.1210/me.2005-0156
A more recent version of this article appeared on December 1, 2005
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Submitted on April 18, 2005
Accepted on June 10, 2005

The Nuclear Xenobiotic Receptor PXR: Recent Insights and New Challenges

Jillian Orans, Denise G. Teotico, and Matthew R. Redinbo*

Department of Chemistry, University of North Carolina at Chapel Hill; Department of Biochemistry and Biophysics, Program in Molecular Biology and Biotechnology, and the Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill

* To whom correspondence should be addressed. E-mail: redinbo{at}unc.edu.

The nuclear receptor PXR plays a key but structurally enigmatic role in human biology. This ligand-regulated transcription factor responds to a diverse array of chemically-distinct ligands, including many endogenous compounds and clinical drugs, and regulates the expression of a critical set of protective gene products involved in xenobiotic and endobiotic metabolism. The structural basis of this receptor's remarkable and unique promiscuity is just now coming into focus. We examine the importance of mobile regions novel to the nuclear receptor ligand binding domain fold in PXR's ability to respond to a variety of small and large agonists. We also review the functional roles played by PXR in numerous biological pathways, and outline emerging areas for the future examination of this key nuclear xenobiotic receptor.

NURSA Molecule Pages Link:

Nuclear Receptors:   SHP  |  TRα  |  TRβ  |  VDR  |  PXR  |  CAR  |  RXRα
Coregulators:   RIP140  |  TRAP220  |  PGC-1  |  TRIP1  |  CARM1  |  SRC-1  |  GRIP1  |  AIB1  |  NCOR  |  SMRT
Ligands:   Rifampicin  |  Pregnenolone carbonitrile  |  Dexamethasone  |  Phenobarbital  |  17β-Estradiol  |  Hyperforin  |  SR12813



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