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Xenoreceptors CAR and PXR activation and consequences on lipid metabolism, glucose homeostasis, and inflammatory response.
Moreau A, Vilarem MJ, Maurel P, Pascussi JM. Moreau A, et al. Mol Pharm. 2008 Jan-Feb;5(1):35-41. doi: 10.1021/mp700103m. Epub 2007 Dec 27. Mol Pharm. 2008. PMID: 18159929 Review.
Xenobiotic and drug metabolism and transport are managed by a large number of genes coordinately regulated by at least three nuclear receptors or xenosensors: aryl hydrocarbon receptor (AhR), constitutive androstane receptor (CAR, NR1I3), and pregnane X receptor (PXR, NR1I …
Xenobiotic and drug metabolism and transport are managed by a large number of genes coordinately regulated by at least three nuclear …
mRNA Expression and Activity of Nucleoside Transporters in Human Hepatoma HepaRG Cells.
Mayati A, Moreau A, Jouan E, Febvre-James M, Denizot C, Parmentier Y, Fardel O. Mayati A, et al. Pharmaceutics. 2018 Nov 21;10(4):246. doi: 10.3390/pharmaceutics10040246. Pharmaceutics. 2018. PMID: 30469356 Free PMC article.
The HepaRG cell line is a highly differentiated human hepatoma cell line, displaying the expression of various drug transporters. However, functional expression of nucleoside transporters remains poorly characterized in HepaRG cells, although these transporters play a
The HepaRG cell line is a highly differentiated human hepatoma cell line, displaying the expression of various drug transporters. How …
Hepatic expression of thyroid hormone-responsive spot 14 protein is regulated by constitutive androstane receptor (NR1I3).
Breuker C, Moreau A, Lakhal L, Tamasi V, Parmentier Y, Meyer U, Maurel P, Lumbroso S, Vilarem MJ, Pascussi JM. Breuker C, et al. Endocrinology. 2010 Apr;151(4):1653-61. doi: 10.1210/en.2009-1435. Epub 2010 Feb 25. Endocrinology. 2010. PMID: 20185760
Deletion or point mutations within this PXR response element led to a drastic inhibition of CAR-mediated THRSP transactivation. ...In conclusion, our results indicate that THRSP gene is a CAR and PXR target gene. Because THRSP expression correlates with lipogenesis …
Deletion or point mutations within this PXR response element led to a drastic inhibition of CAR-mediated THRSP transactivation. ...In …
A novel pregnane X receptor and S14-mediated lipogenic pathway in human hepatocyte.
Moreau A, Téruel C, Beylot M, Albalea V, Tamasi V, Umbdenstock T, Parmentier Y, Sa-Cunha A, Suc B, Fabre JM, Navarro F, Ramos J, Meyer U, Maurel P, Vilarem MJ, Pascussi JM. Moreau A, et al. Hepatology. 2009 Jun;49(6):2068-79. doi: 10.1002/hep.22907. Hepatology. 2009. PMID: 19437491
The pregnane X receptor (PXR) initially isolated as a nuclear receptor regulating xenobiotic and drug metabolism and elimination, seems to play an endobiotic role by affecting lipid homeostasis. ...S14 was first identified as a thyroid-responsive gene and is known t …
The pregnane X receptor (PXR) initially isolated as a nuclear receptor regulating xenobiotic and drug metabolism and elimination, see …
Differential regulation of constitutive androstane receptor expression by hepatocyte nuclear factor4alpha isoforms.
Pascussi JM, Robert A, Moreau A, Ramos J, Bioulac-Sage P, Navarro F, Blanc P, Assenat E, Maurel P, Vilarem MJ. Pascussi JM, et al. Hepatology. 2007 May;45(5):1146-53. doi: 10.1002/hep.21592. Hepatology. 2007. PMID: 17464991
Constitutive androstane receptor (CAR; NR1I3) controls the metabolism and elimination of endogenous and exogenous toxic compounds by up-regulating a battery of genes. ...However, HNF4alpha1 strongly enhanced hCAR promoter activity whereas HNF4alpha7 was a poor activ …
Constitutive androstane receptor (CAR; NR1I3) controls the metabolism and elimination of endogenous and exogenous toxic compounds by up-regu …
Constitutive androstane receptor-vitamin D receptor crosstalk: consequence on CYP24 gene expression.
Moreau A, Maurel P, Vilarem MJ, Pascussi JM. Moreau A, et al. Biochem Biophys Res Commun. 2007 Aug 17;360(1):76-82. doi: 10.1016/j.bbrc.2007.06.003. Epub 2007 Jun 13. Biochem Biophys Res Commun. 2007. PMID: 17585873
The current study shows that: (i) CAR-RXR heterodimer binds to and transactivates the proximal promoter of CYP24 (-1200/+22) and both VDRE-1 and VDRE-2 which control its expression in response to 1,25-dihydroxyvitamin D(3), (ii) androstanol an inverse agonist of hCAR inhibits tra …
The current study shows that: (i) CAR-RXR heterodimer binds to and transactivates the proximal promoter of CYP24 (-1200/+22) and both VDRE-1 …
Metabonomic studies on human hepatocyte in primary culture.
Croixmarie V, Umbdenstock T, Cloarec O, Moreau A, Pascussi JM, Parmentier Y, Boursier-Neyret C, Walther B. Croixmarie V, et al. Methods Mol Biol. 2010;640:355-74. doi: 10.1007/978-1-60761-688-7_19. Methods Mol Biol. 2010. PMID: 20645062
Mechanisms involved in induction processes have been investigated using fresh human hepatocytes in culture as a cellular model and using mass spectrometry-based metabonomics as a global investigation tool. ...Rifampicin, a nuclear pregnane X receptor (PXR) li …
Mechanisms involved in induction processes have been investigated using fresh human hepatocytes in culture as a cellular model and us …
Functionalized PLA-PEG nanoparticles targeting intestinal transporter PepT1 for oral delivery of acyclovir.
Gourdon B, Chemin C, Moreau A, Arnauld T, Baumy P, Cisternino S, Péan JM, Declèves X. Gourdon B, et al. Int J Pharm. 2017 Aug 30;529(1-2):357-370. doi: 10.1016/j.ijpharm.2017.07.024. Epub 2017 Jul 10. Int J Pharm. 2017. PMID: 28705621
Targeting intestinal di- and tri-peptide transporter PepT1 with prodrugs is a successful strategy to improve oral drug bioavailability, as demonstrated with valacyclovir, a prodrug of acyclovir. ...Acyclovir was encapsulated with a drug load of ≈10% in valine …
Targeting intestinal di- and tri-peptide transporter PepT1 with prodrugs is a successful strategy to improve oral drug bioavailabilit …
Effect of Gevokizumab on Interleukin-1β-Mediated Cytochrome P450 3A4 and Drug Transporter Repression in Cultured Human Hepatocytes.
Moreau A, Le Vée M, Jouan E, Denizot C, Parmentier Y, Fardel O. Moreau A, et al. Eur J Drug Metab Pharmacokinet. 2017 Oct;42(5):871-878. doi: 10.1007/s13318-017-0406-1. Eur J Drug Metab Pharmacokinet. 2017. PMID: 28260174
BACKGROUND AND OBJECTIVES: Gevokizumab is a potent anti-interleukin (IL)-1β neutralizing monoclonal antibody (mAb), which may be used for treating inflammatory or autoimmune diseases. ...CONCLUSION: Gevokizumab attenuates, but not abolishes, IL-1β-mediated functional repre …
BACKGROUND AND OBJECTIVES: Gevokizumab is a potent anti-interleukin (IL)-1β neutralizing monoclonal antibody (mAb), which may be used …
Drug transporter expression in human macrophages.
Moreau A, Le Vee M, Jouan E, Parmentier Y, Fardel O. Moreau A, et al. Fundam Clin Pharmacol. 2011 Dec;25(6):743-52. doi: 10.1111/j.1472-8206.2010.00913.x. Epub 2011 Jan 7. Fundam Clin Pharmacol. 2011. PMID: 21210849
Such a functional expression of these transporters has likely to be considered with respect to cellular pharmacokinetics of drugs targeting macrophages....
Such a functional expression of these transporters has likely to be considered with respect to cellular pharmacokinetics of drugs tar …
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