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Di(2-ethylhexyl) phthalate is a highly potent agonist for the human constitutive androstane receptor splice variant CAR2.

DeKeyser JG, Stagliano MC, Auerbach SS, Prabhu KS, Jones AD, Omiecinski CJ.

Mol Pharmacol. 2009 May;75(5):1005-13. doi: 10.1124/mol.108.053702. Epub 2009 Feb 11.


Structure-Dependent Activity of Phthalate Esters and Phthalate Monoesters Binding to Human Constitutive Androstane Receptor.

Zhang H, Zhang Z, Nakanishi T, Wan Y, Hiromori Y, Nagase H, Hu J.

Chem Res Toxicol. 2015 Jun 15;28(6):1196-204. doi: 10.1021/acs.chemrestox.5b00028. Epub 2015 May 13.


Nigramide J is a novel potent inverse agonist of the human constitutive androstane receptor.

Kanno Y, Tanuma N, Yatsu T, Li W, Koike K, Inouye Y.

Pharmacol Res Perspect. 2014 Feb;2(1):2. doi: 10.1002/prp2.18. Epub 2014 Jan 26.


Editorial expression of concern: Enhancing nuclear receptor-induced transcription requires nuclear motor and LSD1-dependent gene networking in interchromatin granules.

Verma IM.

Proc Natl Acad Sci U S A. 2014 Sep 9;111(36):13241. doi: 10.1073/pnas.1415649111. Epub 2014 Sep 2. No abstract available.


Human receptor activation by aroclor 1260, a polychlorinated biphenyl mixture.

Wahlang B, Falkner KC, Clair HB, Al-Eryani L, Prough RA, States JC, Coslo DM, Omiecinski CJ, Cave MC.

Toxicol Sci. 2014 Aug 1;140(2):283-97. doi: 10.1093/toxsci/kfu083. Epub 2014 May 8.


Evidence for triclosan-induced activation of human and rodent xenobiotic nuclear receptors.

Paul KB, Thompson JT, Simmons SO, Vanden Heuvel JP, Crofton KM.

Toxicol In Vitro. 2013 Oct;27(7):2049-60. doi: 10.1016/j.tiv.2013.07.008. Epub 2013 Jul 27.


TO901317, a potent LXR agonist, is an inverse agonist of CAR.

Kanno Y, Tanuma N, Takahashi A, Inouye Y.

J Toxicol Sci. 2013;38(3):309-15.


Coordinated roles of pregnane X receptor and constitutive androstane receptor in autoinduction of voriconazole metabolism in mice.

Ohbuchi M, Yoshinari K, Kaneko H, Matsumoto S, Inoue A, Kawamura A, Usui T, Yamazoe Y.

Antimicrob Agents Chemother. 2013 Mar;57(3):1332-8. doi: 10.1128/AAC.01900-12. Epub 2012 Dec 28.


Evaluation of Ginkgo biloba extract as an activator of human glucocorticoid receptor.

Lau AJ, Yang G, Rajaraman G, Baucom CC, Chang TK.

J Ethnopharmacol. 2013 Jan 30;145(2):670-5. doi: 10.1016/j.jep.2012.11.038. Epub 2012 Dec 5.


Identification of novel activators of constitutive androstane receptor from FDA-approved drugs by integrated computational and biological approaches.

Lynch C, Pan Y, Li L, Ferguson SS, Xia M, Swaan PW, Wang H.

Pharm Res. 2013 Feb;30(2):489-501. doi: 10.1007/s11095-012-0895-1. Epub 2012 Oct 23.


The orphan nuclear receptor DAX-1 functions as a potent corepressor of the constitutive androstane receptor (NR1I3).

Laurenzana EM, Chen T, Kannuswamy M, Sell BE, Strom SC, Li Y, Omiecinski CJ.

Mol Pharmacol. 2012 Nov;82(5):918-28. doi: 10.1124/mol.112.080721. Epub 2012 Aug 15.


Differential effects of clinically used derivatives and metabolites of artemisinin in the activation of constitutive androstane receptor isoforms.

Burk O, Piedade R, Ghebreghiorghis L, Fait JT, Nussler AK, Gil JP, Windshügel B, Schwab M.

Br J Pharmacol. 2012 Oct;167(3):666-81. doi: 10.1111/j.1476-5381.2012.02033.x.


Effects of atorvastatin metabolites on induction of drug-metabolizing enzymes and membrane transporters through human pregnane X receptor.

Hoffart E, Ghebreghiorghis L, Nussler AK, Thasler WE, Weiss TS, Schwab M, Burk O.

Br J Pharmacol. 2012 Mar;165(5):1595-608. doi: 10.1111/j.1476-5381.2011.01665.x.


Isoform-selective activation of human constitutive androstane receptor by Ginkgo biloba extract: functional analysis of the SV23, SV24, and SV25 splice variants.

Lau AJ, Yang G, Chang TK.

J Pharmacol Exp Ther. 2011 Nov;339(2):704-15. doi: 10.1124/jpet.111.186130. Epub 2011 Aug 23.


Multi-species analyses of direct activators of the constitutive androstane receptor.

Omiecinski CJ, Coslo DM, Chen T, Laurenzana EM, Peffer RC.

Toxicol Sci. 2011 Oct;123(2):550-62. doi: 10.1093/toxsci/kfr191. Epub 2011 Jul 21.


The role of constitutive androstane receptor in oxazaphosphorine-mediated induction of drug-metabolizing enzymes in human hepatocytes.

Wang D, Li L, Fuhrman J, Ferguson S, Wang H.

Pharm Res. 2011 Aug;28(8):2034-44. doi: 10.1007/s11095-011-0429-2. Epub 2011 Apr 13.


Modulation of constitutive androstane receptor (CAR) and pregnane X receptor (PXR) by 6-arylpyrrolo[2,1-d][1,5]benzothiazepine derivatives, ligands of peripheral benzodiazepine receptor (PBR).

Anderson LE, Dring AM, Hamel LD, Stoner MA.

Toxicol Lett. 2011 Apr 25;202(2):148-54. doi: 10.1016/j.toxlet.2011.02.004. Epub 2011 Feb 18.


Selective phthalate activation of naturally occurring human constitutive androstane receptor splice variants and the pregnane X receptor.

DeKeyser JG, Laurenzana EM, Peterson EC, Chen T, Omiecinski CJ.

Toxicol Sci. 2011 Apr;120(2):381-91. doi: 10.1093/toxsci/kfq394. Epub 2011 Jan 12.


Differential activation of pregnane X receptor and constitutive androstane receptor by buprenorphine in primary human hepatocytes and HepG2 cells.

Li L, Hassan HE, Tolson AH, Ferguson SS, Eddington ND, Wang H.

J Pharmacol Exp Ther. 2010 Dec;335(3):562-71. doi: 10.1124/jpet.110.173187. Epub 2010 Sep 9.


Endosulfan induces CYP2B6 and CYP3A4 by activating the pregnane X receptor.

Casabar RC, Das PC, Dekrey GK, Gardiner CS, Cao Y, Rose RL, Wallace AD.

Toxicol Appl Pharmacol. 2010 Jun 15;245(3):335-43. doi: 10.1016/j.taap.2010.03.017. Epub 2010 Mar 31.

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