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Vol. 62, Issue 3, 638-646, September 2002
Nuclear Receptor Discovery Research (J.M.M., C.M.S., B.G., J.T.M.,
S.A.K.) and Bioscience Support (D.H.-B.), GlaxoSmithKline, Research
Triangle Park, North Carolina
The nuclear pregnane X receptor (PXR) and constitutive androstane
receptor (CAR) play central roles in protecting the body against
environmental chemicals (xenobiotics). PXR and CAR are activated by a
wide range of xenobiotics and regulate cytochrome P450 and other genes
whose products are involved in the detoxification of these chemicals.
In this report, we have used receptor-selective agonists together with
receptor-null mice to identify PXR and CAR target genes in the liver
and small intestine. Our results demonstrate that PXR and CAR regulate
overlapping but distinct sets of genes involved in all phases of
xenobiotic metabolism, including oxidative metabolism, conjugation, and
transport. Among the murine genes regulated by PXR were those encoding
PXR and CAR. We provide evidence that PXR regulates a similar program of genes involved in xenobiotic metabolism in human liver. Among the
genes regulated by PXR in primary human hepatocytes were the aryl
hydrocarbon receptor and its target genes CYP1A1 and
CYP1A2. These findings underscore the importance of
these two nuclear receptors in defending the body against a broad array
of potentially harmful xenobiotics.
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W. Huang, J. Zhang, P. Wei, W. T. Schrader, and D. D. Moore Meclizine Is an Agonist Ligand for Mouse Constitutive Androstane Receptor (CAR) and an Inverse Agonist for Human CAR Mol. Endocrinol., October 1, 2004; 18(10): 2402 - 2408. [Abstract] [Full Text] [PDF] |
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S. Kodama, C. Koike, M. Negishi, and Y. Yamamoto Nuclear Receptors CAR and PXR Cross Talk with FOXO1 To Regulate Genes That Encode Drug-Metabolizing and Gluconeogenic Enzymes Mol. Cell. Biol., September 15, 2004; 24(18): 7931 - 7940. [Abstract] [Full Text] [PDF] |
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C. J. Matheny, R. Y. Ali, X. Yang, and G. M. Pollack EFFECT OF PROTOTYPICAL INDUCING AGENTS ON P-GLYCOPROTEIN AND CYP3A EXPRESSION IN MOUSE TISSUES Drug Metab. Dispos., September 1, 2004; 32(9): 1008 - 1014. [Abstract] [Full Text] [PDF] |
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K. Swales and M. Negishi CAR, Driving into the Future Mol. Endocrinol., July 1, 2004; 18(7): 1589 - 1598. [Abstract] [Full Text] [PDF] |
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M. Podvinec, C. Handschin, R. Looser, and U. A. Meyer Identification of the xenosensors regulating human 5-aminolevulinate synthase PNAS, June 15, 2004; 101(24): 9127 - 9132. [Abstract] [Full Text] [PDF] |
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J. M. Maglich, J. Watson, P. J. McMillen, B. Goodwin, T. M. Willson, and J. T. Moore The Nuclear Receptor CAR Is a Regulator of Thyroid Hormone Metabolism during Caloric Restriction J. Biol. Chem., May 7, 2004; 279(19): 19832 - 19838. [Abstract] [Full Text] [PDF] |
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V. Bombail, K. Taylor, G. G. Gibson, and N. Plant ROLE OF Sp1, C/EBP{alpha}, HNF3, AND PXR IN THE BASAL- AND XENOBIOTIC-MEDIATED REGULATION OF THE CYP3A4 GENE Drug Metab. Dispos., May 1, 2004; 32(5): 525 - 535. [Abstract] [Full Text] [PDF] |
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D. P. Hartley, X. Dai, Y. D. He, E. J. Carlini, B. Wang, S.-e. W. Huskey, R. G. Ulrich, T. H. Rushmore, R. Evers, and D. C. Evans Activators of the Rat Pregnane X Receptor Differentially Modulate Hepatic and Intestinal Gene Expression Mol. Pharmacol., May 1, 2004; 65(5): 1159 - 1171. [Abstract] [Full Text] |
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S. D. Shenoy, T. A. Spencer, N. A. Mercer-Haines, M. Abdolalipour, W. L. Wurster, M. Runge-Morris, and T. A. Kocarek Induction of CYP3A by 2,3-Oxidosqualene:Lanosterol Cyclase Inhibitors Is Mediated by an Endogenous Squalene Metabolite in Primary Cultured Rat Hepatocytes Mol. Pharmacol., May 1, 2004; 65(5): 1302 - 1312. [Abstract] [Full Text] |
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Z. Zhang, P. E. Burch, A. J. Cooney, R. B. Lanz, F. A. Pereira, J. Wu, R. A. Gibbs, G. Weinstock, and D. A. Wheeler Genomic Analysis of the Nuclear Receptor Family: New Insights Into Structure, Regulation, and Evolution From the Rat Genome Genome Res., April 1, 2004; 14(4): 580 - 590. [Abstract] [Full Text] [PDF] |
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C. Stedman, G. Robertson, S. Coulter, and C. Liddle Feed-forward Regulation of Bile Acid Detoxification by CYP3A4: STUDIES IN HUMANIZED TRANSGENIC MICE J. Biol. Chem., March 19, 2004; 279(12): 11336 - 11343. [Abstract] [Full Text] [PDF] |
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S. P. S. Saini, J. Sonoda, L. Xu, D. Toma, H. Uppal, Y. Mu, S. Ren, D. D. Moore, R. M. Evans, and W. Xie A Novel Constitutive Androstane Receptor-Mediated and CYP3A-Independent Pathway of Bile Acid Detoxification Mol. Pharmacol., February 1, 2004; 65(2): 292 - 300. [Abstract] [Full Text] [PDF] |
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C G Dietrich, A Geier, and R P J Oude Elferink ABC of oral bioavailability: transporters as gatekeepers in the gut Gut, December 1, 2003; 52(12): 1788 - 1795. [Full Text] [PDF] |
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C. Handschin and U. A. Meyer Induction of Drug Metabolism: The Role of Nuclear Receptors Pharmacol. Rev., December 1, 2003; 55(4): 649 - 673. [Abstract] [Full Text] [PDF] |
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G. L. Guo, G. Lambert, M. Negishi, J. M. Ward, H. B. Brewer Jr., S. A. Kliewer, F. J. Gonzalez, and C. J. Sinal Complementary Roles of Farnesoid X Receptor, Pregnane X Receptor, and Constitutive Androstane Receptor in Protection against Bile Acid Toxicity J. Biol. Chem., November 14, 2003; 278(46): 45062 - 45071. [Abstract] [Full Text] [PDF] |
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S. Teng, V. Jekerle, and M. Piquette-Miller INDUCTION OF ABCC3 (MRP3) BY PREGNANE X RECEPTOR ACTIVATORS Drug Metab. Dispos., November 1, 2003; 31(11): 1296 - 1299. [Abstract] [Full Text] [PDF] |
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N. J. Cherrington, A. L. Slitt, J. M. Maher, X.-X. Zhang, J. Zhang, W. Huang, Y.-J. Y. Wan, D. D. Moore, and C. D. Klaassen INDUCTION OF MULTIDRUG RESISTANCE PROTEIN 3 (MRP3) IN VIVO IS INDEPENDENT OF CONSTITUTIVE ANDROSTANE RECEPTOR Drug Metab. Dispos., November 1, 2003; 31(11): 1315 - 1319. [Abstract] [Full Text] [PDF] |
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D. J. Fraser, A. Zumsteg, and U. A. Meyer Nuclear Receptors Constitutive Androstane Receptor and Pregnane X Receptor Activate a Drug-responsive Enhancer of the Murine 5-Aminolevulinic Acid Synthase Gene J. Biol. Chem., October 10, 2003; 278(41): 39392 - 39401. [Abstract] [Full Text] [PDF] |
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C. Chen, J. L. Staudinger, and C. D. Klaassen NUCLEAR RECEPTOR, PREGNANE X RECEPTOR, IS REQUIRED FOR INDUCTION OF UDP-GLUCURONOSYLTRANSFERASES IN MOUSE LIVER BY PREGNENOLONE-16{alpha}-CARBONITRILE Drug Metab. Dispos., July 1, 2003; 31(7): 908 - 915. [Abstract] [Full Text] [PDF] |
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J. M. Rosenfeld, R. Vargas Jr., W. Xie, and R. M. Evans Genetic Profiling Defines the Xenobiotic Gene Network Controlled by the Nuclear Receptor Pregnane X Receptor Mol. Endocrinol., July 1, 2003; 17(7): 1268 - 1282. [Abstract] [Full Text] [PDF] |
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S. A. Kliewer The Nuclear Pregnane X Receptor Regulates Xenobiotic Detoxification J. Nutr., July 1, 2003; 133(7): 2444S - 2447. [Abstract] [Full Text] [PDF] |
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S. S. Auerbach, R. Ramsden, M. A. Stoner, C. Verlinde, C. Hassett, and C. J. Omiecinski Alternatively spliced isoforms of the human constitutive androstane receptor Nucleic Acids Res., June 15, 2003; 31(12): 3194 - 3207. [Abstract] [Full Text] [PDF] |
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J. M. Maglich, D. J. Parks, L. B. Moore, J. L. Collins, B. Goodwin, A. N. Billin, C. A. Stoltz, S. A. Kliewer, M. H. Lambert, T. M. Willson, et al. Identification of a Novel Human Constitutive Androstane Receptor (CAR) Agonist and Its Use in the Identification of CAR Target Genes J. Biol. Chem., May 2, 2003; 278(19): 17277 - 17283. [Abstract] [Full Text] [PDF] |
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J. L. Staudinger, A. Madan, K. M. Carol, and A. Parkinson Regulation of Drug Transporter Gene Expression by Nuclear Receptors Drug Metab. Dispos., May 1, 2003; 31(5): 523 - 527. [Abstract] [Full Text] [PDF] |
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W. Xie, M.-F. Yeuh, A. Radominska-Pandya, S. P. S. Saini, Y. Negishi, B. S. Bottroff, G. Y. Cabrera, R. H. Tukey, and R. M. Evans Control of steroid, heme, and carcinogen metabolism by nuclear pregnane X receptor and constitutive androstane receptor PNAS, April 1, 2003; 100(7): 4150 - 4155. [Abstract] [Full Text] [PDF] |
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W. Huang, J. Zhang, S. S. Chua, M. Qatanani, Y. Han, R. Granata, and D. D. Moore Induction of bilirubin clearance by the constitutive androstane receptor (CAR) PNAS, April 1, 2003; 100(7): 4156 - 4161. [Abstract] [Full Text] [PDF] |
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I. Dussault, H.-D. Yoo, M. Lin, E. Wang, M. Fan, A. K. Batta, G. Salen, S. K. Erickson, and B. M. Forman Identification of an endogenous ligand that activates pregnane X receptor-mediated sterol clearance PNAS, February 4, 2003; 100(3): 833 - 838. [Abstract] [Full Text] [PDF] |
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B. Goodwin, K. C. Gauthier, M. Umetani, M. A. Watson, M. I. Lochansky, J. L. Collins, E. Leitersdorf, D. J. Mangelsdorf, S. A. Kliewer, and J. J. Repa Identification of bile acid precursors as endogenous ligands for the nuclear xenobiotic pregnane X receptor PNAS, January 7, 2003; 100(1): 223 - 228. [Abstract] [Full Text] [PDF] |
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S. A. Kliewer, B. Goodwin, and T. M. Willson The Nuclear Pregnane X Receptor: A Key Regulator of Xenobiotic Metabolism Endocr. Rev., October 1, 2002; 23(5): 687 - 702. [Abstract] [Full Text] [PDF] |
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