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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

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