This Article Full Text Full Text (PDF) All Versions of this Article: 19/12/2891    most recent Author Manuscript (PDF) Purchase Article View Shopping Cart Alert me when this article is cited Alert me if a correction is posted Citation Map Services Email this article to a friend Similar articles in this journal Similar articles in PubMed Alert me to new issues of the journal Download to citation manager NURSA Molecule Pages Link Citing Articles Citing Articles via HighWire Citing Articles via Google Scholar Google Scholar Articles by Orans, J. Articles by Redinbo, M. R. Search for Related Content PubMed PubMed Citation Articles by Orans, J. Articles by Redinbo, M. R.

The Nuclear Xenobiotic Receptor Pregnane X Receptor: Recent Insights and New Challenges

Department of Chemistry (J.O., D.G.T., M.R.R.) and Department of Biochemistry and Biophysics, Program in Molecular Biology and Biotechnology, and the Lineberger Comprehensive Cancer Center (M.R.R.), University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599-3290

Address all correspondence and requests for reprints to: Matthew R. Redinbo, Ph.D., Department of Chemistry, CB 3290, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599-3290. E-mail: redinbo{at}unc.edu.

The nuclear receptor pregnane X 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 the ability of PXR 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

This article has been cited by other articles:

				G. Lemaire, C. Benod, V. Nahoum, A. Pillon, A.-M. Boussioux, J.-F. Guichou, G. Subra, J.-M. Pascussi, W. Bourguet, A. Chavanieu, et al. Discovery of a Highly Active Ligand of Human Pregnane X Receptor: A Case Study from Pharmacophore Modeling and Virtual Screening to "In Vivo" Biological Activity Mol. Pharmacol., September 1, 2007; 72(3): 572 - 581. [Abstract] [Full Text] [PDF]

				Y. Xue, L. B. Moore, J. Orans, L. Peng, S. Bencharit, S. A. Kliewer, and M. R. Redinbo Crystal Structure of the Pregnane X Receptor-Estradiol Complex Provides Insights into Endobiotic Recognition Mol. Endocrinol., May 1, 2007; 21(5): 1028 - 1038. [Abstract] [Full Text] [PDF]

				I. M. Medina-Diaz, G. Arteaga-Illan, M. B. de Leon, B. Cisneros, A. Sierra-Santoyo, L. Vega, F. J. Gonzalez, and G. Elizondo Pregnane X Receptor-Dependent Induction of the CYP3A4 Gene by o,p'-1,1,1,-Trichloro-2,2-Bis (p-Chlorophenyl)ethane Drug Metab. Dispos., January 1, 2007; 35(1): 95 - 102. [Abstract] [Full Text] [PDF]

				J. Guzelian, J. L. Barwick, L. Hunter, T. L. Phang, L. C. Quattrochi, and P. S. Guzelian Identification of Genes Controlled by the Pregnane X Receptor by Microarray Analysis of mRNAs from Pregnenolone 16{alpha}-Carbonitrile-Treated Rats Toxicol. Sci., December 1, 2006; 94(2): 379 - 387. [Abstract] [Full Text] [PDF]