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Expansion of human primary hepatocytes in vitro through their amplification as liver progenitors in a 3D organoid system.

Garnier D, Li R, Delbos F, Fourrier A, Collet C, Guguen-Guillouzo C, Chesné C, Nguyen TH.

Sci Rep. 2018 May 29;8(1):8222. doi: 10.1038/s41598-018-26584-1.


Endoplasmic reticulum stress precedes oxidative stress in antibiotic-induced cholestasis and cytotoxicity in human hepatocytes.

Burban A, Sharanek A, Guguen-Guillouzo C, Guillouzo A.

Free Radic Biol Med. 2018 Feb 1;115:166-178. doi: 10.1016/j.freeradbiomed.2017.11.017. Epub 2017 Dec 2.


Progressive and Preferential Cellular Accumulation of Hydrophobic Bile Acids Induced by Cholestatic Drugs Is Associated with Inhibition of Their Amidation and Sulfation.

Sharanek A, Burban A, Humbert L, Guguen-Guillouzo C, Rainteau D, Guillouzo A.

Drug Metab Dispos. 2017 Dec;45(12):1292-1303. doi: 10.1124/dmd.117.077420. Epub 2017 Sep 19.


Penicillinase-resistant antibiotics induce non-immune-mediated cholestasis through HSP27 activation associated with PKC/P38 and PI3K/AKT signaling pathways.

Burban A, Sharanek A, Hüe R, Gay M, Routier S, Guillouzo A, Guguen-Guillouzo C.

Sci Rep. 2017 May 12;7(1):1815. doi: 10.1038/s41598-017-01171-y.


From the Cover: MechanisticInsights in Cytotoxic and Cholestatic Potential of the Endothelial Receptor Antagonists Using HepaRG Cells.

Burbank MG, Sharanek A, Burban A, Mialanne H, Aerts H, Guguen-Guillouzo C, Weaver RJ, Guillouzo A.

Toxicol Sci. 2017 Jun 1;157(2):451-464. doi: 10.1093/toxsci/kfx062.


Early Alterations of Bile Canaliculi Dynamics and the Rho Kinase/Myosin Light Chain Kinase Pathway Are Characteristics of Drug-Induced Intrahepatic Cholestasis.

Burbank MG, Burban A, Sharanek A, Weaver RJ, Guguen-Guillouzo C, Guillouzo A.

Drug Metab Dispos. 2016 Nov;44(11):1780-1793. Epub 2016 Aug 18.


Differential sensitivity of metabolically competent and non-competent HepaRG cells to apoptosis induced by diclofenac combined or not with TNF-α.

Al-Attrache H, Sharanek A, Burban A, Burbank M, Gicquel T, Abdel-Razzak Z, Guguen-Guillouzo C, Morel I, Guillouzo A.

Toxicol Lett. 2016 Sep 6;258:71-86. doi: 10.1016/j.toxlet.2016.06.008. Epub 2016 Jun 14.


Rho-kinase/myosin light chain kinase pathway plays a key role in the impairment of bile canaliculi dynamics induced by cholestatic drugs.

Sharanek A, Burban A, Burbank M, Le Guevel R, Li R, Guillouzo A, Guguen-Guillouzo C.

Sci Rep. 2016 May 12;6:24709. doi: 10.1038/srep24709.


Novel optimization of valmerins (tetrahydropyrido[1,2-a]isoindolones) as potent dual CDK5/GSK3 inhibitors.

Ouach A, Boulahjar R, Vala C, Bourg S, Bonnet P, Guguen-Guillouzo C, Ravache M, Le Guevel R, Lozach O, Lazar S, Troin Y, Meijer L, Ruchaud S, Akssira M, Guillaumet G, Routier S.

Eur J Med Chem. 2016 Jun 10;115:311-25. doi: 10.1016/j.ejmech.2016.02.072. Epub 2016 Mar 2.


Hepatic differentiation of human pluripotent stem cells on human liver progenitor HepaRG-derived acellular matrix.

Kanninen LK, Porola P, Niklander J, Malinen MM, Corlu A, Guguen-Guillouzo C, Urtti A, Yliperttula ML, Lou YR.

Exp Cell Res. 2016 Feb 15;341(2):207-17. doi: 10.1016/j.yexcr.2016.02.006. Epub 2016 Feb 8.


Functional polymer-dependent 3D culture accelerates the differentiation of HepaRG cells into mature hepatocytes.

Higuchi Y, Kawai K, Kanaki T, Yamazaki H, Chesné C, Guguen-Guillouzo C, Suemizu H.

Hepatol Res. 2016 Sep;46(10):1045-57. doi: 10.1111/hepr.12644. Epub 2016 Feb 7.


Two persistent organic pollutants which act through different xenosensors (alpha-endosulfan and 2,3,7,8 tetrachlorodibenzo-p-dioxin) interact in a mixture and downregulate multiple genes involved in human hepatocyte lipid and glucose metabolism.

Ambolet-Camoit A, Ottolenghi C, Leblanc A, Kim MJ, Letourneur F, Jacques S, Cagnard N, Guguen-Guillouzo C, Barouki R, Aggerbeck M.

Biochimie. 2015 Sep;116:79-91. doi: 10.1016/j.biochi.2015.07.003. Epub 2015 Jul 6.


Advances in tetrahydropyrido[1,2-a]isoindolone (valmerins) series: Potent glycogen synthase kinase 3 and cyclin dependent kinase 5 inhibitors.

Boulahjar R, Ouach A, Bourg S, Bonnet P, Lozach O, Meijer L, Guguen-Guillouzo C, Le Guevel R, Lazar S, Akssira M, Troin Y, Guillaumet G, Routier S.

Eur J Med Chem. 2015 Aug 28;101:274-87. doi: 10.1016/j.ejmech.2015.06.046. Epub 2015 Jun 27.


Comparative Localization and Functional Activity of the Main Hepatobiliary Transporters in HepaRG Cells and Primary Human Hepatocytes.

Bachour-El Azzi P, Sharanek A, Burban A, Li R, Guével RL, Abdel-Razzak Z, Stieger B, Guguen-Guillouzo C, Guillouzo A.

Toxicol Sci. 2015 May;145(1):157-68. doi: 10.1093/toxsci/kfv041. Epub 2015 Feb 17.


Liver X receptor α (LXRα/NR1H3) regulates differentiation of hepatocyte-like cells via reciprocal regulation of HNF4α.

Chen KT, Pernelle K, Tsai YH, Wu YH, Hsieh JY, Liao KH, Guguen-Guillouzo C, Wang HW.

J Hepatol. 2014 Dec;61(6):1276-86. doi: 10.1016/j.jhep.2014.07.025. Epub 2014 Jul 27.


Impact of inflammation on chlorpromazine-induced cytotoxicity and cholestatic features in HepaRG cells.

Bachour-El Azzi P, Sharanek A, Abdel-Razzak Z, Antherieu S, Al-Attrache H, Savary CC, Lepage S, Morel I, Labbe G, Guguen-Guillouzo C, Guillouzo A.

Drug Metab Dispos. 2014 Sep;42(9):1556-66. doi: 10.1124/dmd.114.058123. Epub 2014 Jul 7.


Different dose-dependent mechanisms are involved in early cyclosporine a-induced cholestatic effects in hepaRG cells.

Sharanek A, Azzi PB, Al-Attrache H, Savary CC, Humbert L, Rainteau D, Guguen-Guillouzo C, Guillouzo A.

Toxicol Sci. 2014 Sep;141(1):244-53. doi: 10.1093/toxsci/kfu122. Epub 2014 Jun 27.


The human hepatic cell line HepaRG as a possible cell source for the generation of humanized liver TK-NOG mice.

Higuchi Y, Kawai K, Yamazaki H, Nakamura M, Bree F, Guguen-Guillouzo C, Suemizu H.

Xenobiotica. 2014 Jan;44(2):146-53. doi: 10.3109/00498254.2013.836257. Epub 2013 Sep 25.


Oxidative stress plays a major role in chlorpromazine-induced cholestasis in human HepaRG cells.

Anthérieu S, Bachour-El Azzi P, Dumont J, Abdel-Razzak Z, Guguen-Guillouzo C, Fromenty B, Robin MA, Guillouzo A.

Hepatology. 2013 Apr;57(4):1518-29. doi: 10.1002/hep.26160. Epub 2013 Mar 4.


Combined Stimulation with the Tumor Necrosis Factor α and the Epidermal Growth Factor Promotes the Proliferation of Hepatocytes in Rat Liver Cultured Slices.

Finot F, Masson R, Desmots F, Ribault C, Bichet N, Vericat JA, Lafouge P, Guguen-Guillouzo C, Loyer P.

Int J Hepatol. 2012;2012:785786. doi: 10.1155/2012/785786. Epub 2012 Oct 16.


Novel tetrahydropyrido[1,2-a]isoindolone derivatives (valmerins): potent cyclin-dependent kinase/glycogen synthase kinase 3 inhibitors with antiproliferative activities and antitumor effects in human tumor xenografts.

Boulahjar R, Ouach A, Matteo C, Bourg S, Ravache M, le Guével R, Marionneau S, Oullier T, Lozach O, Meijer L, Guguen-Guillouzo C, Lazar S, Akssira M, Troin Y, Guillaumet G, Routier S.

J Med Chem. 2012 Nov 26;55(22):9589-606. doi: 10.1021/jm3008536. Epub 2012 Nov 1.


Three-dimensional HepaRG model as an attractive tool for toxicity testing.

Leite SB, Wilk-Zasadna I, Zaldivar JM, Airola E, Reis-Fernandes MA, Mennecozzi M, Guguen-Guillouzo C, Chesne C, Guillou C, Alves PM, Coecke S.

Toxicol Sci. 2012 Nov;130(1):106-16. doi: 10.1093/toxsci/kfs232. Epub 2012 Jul 27.


Nanofibrillar cellulose hydrogel promotes three-dimensional liver cell culture.

Bhattacharya M, Malinen MM, Lauren P, Lou YR, Kuisma SW, Kanninen L, Lille M, Corlu A, GuGuen-Guillouzo C, Ikkala O, Laukkanen A, Urtti A, Yliperttula M.

J Control Release. 2012 Dec 28;164(3):291-8. doi: 10.1016/j.jconrel.2012.06.039. Epub 2012 Jul 7.


Optimization of the HepaRG cell model for drug metabolism and toxicity studies.

Anthérieu S, Chesné C, Li R, Guguen-Guillouzo C, Guillouzo A.

Toxicol In Vitro. 2012 Dec;26(8):1278-85. doi: 10.1016/j.tiv.2012.05.008. Epub 2012 May 27. Review.


Co-cultures of enterocytes and hepatocytes for retinoid transport and metabolism.

Rossi C, Guantario B, Ferruzza S, Guguen-Guillouzo C, Sambuy Y, Scarino ML, Bellovino D.

Toxicol In Vitro. 2012 Dec;26(8):1256-64. doi: 10.1016/j.tiv.2012.04.013. Epub 2012 Apr 20.


CYP4F3B expression is associated with differentiation of HepaRG human hepatocytes and unaffected by fatty acid overload.

Madec S, Cerec V, Plée-Gautier E, Antoun J, Glaise D, Salaun JP, Guguen-Guillouzo C, Corlu A.

Drug Metab Dispos. 2011 Oct;39(10):1987-96. doi: 10.1124/dmd.110.036848. Epub 2011 Jul 21.


Automated detection of hepatotoxic compounds in human hepatocytes using HepaRG cells and image-based analysis of mitochondrial dysfunction with JC-1 dye.

Pernelle K, Le Guevel R, Glaise D, Stasio CG, Le Charpentier T, Bouaita B, Corlu A, Guguen-Guillouzo C.

Toxicol Appl Pharmacol. 2011 Aug 1;254(3):256-66. doi: 10.1016/j.taap.2011.04.018. Epub 2011 May 4.


The promoter of human telomerase reverse transcriptase is activated during liver regeneration and hepatocyte proliferation.

Sirma H, Kumar M, Meena JK, Witt B, Weise JM, Lechel A, Ande S, Sakk V, Guguen-Guillouzo C, Zender L, Rudolph KL, Günes C.

Gastroenterology. 2011 Jul;141(1):326-37, 337.e1-3. doi: 10.1053/j.gastro.2011.03.047. Epub 2011 Mar 27.


Electrochemical synthesis and characterisation of alternating tripyridyl-dipyrrole molecular strands with multiple nitrogen-based donor-acceptor binding sites.

Tabatchnik-Rebillon A, Aubé C, Bakkali H, Delaunay T, Manh GT, Blot V, Thobie-Gautier C, Renault E, Soulard M, Planchat A, Le Questel JY, Le Guével R, Guguen-Guillouzo C, Kauffmann B, Ferrand Y, Huc I, Urgin K, Condon S, Léonel E, Evain M, Lebreton J, Jacquemin D, Pipelier M, Dubreuil D.

Chemistry. 2010 Oct 18;16(39):11876-89. doi: 10.1002/chem.201000859.


Assessment of the genotoxic potential of indirect chemical mutagens in HepaRG cells by the comet and the cytokinesis-block micronucleus assays.

Le Hegarat L, Dumont J, Josse R, Huet S, Lanceleur R, Mourot A, Poul JM, Guguen-Guillouzo C, Guillouzo A, Fessard V.

Mutagenesis. 2010 Nov;25(6):555-60. doi: 10.1093/mutage/geq039. Epub 2010 Jul 30.


General review on in vitro hepatocyte models and their applications.

Guguen-Guillouzo C, Guillouzo A.

Methods Mol Biol. 2010;640:1-40. doi: 10.1007/978-1-60761-688-7_1. Review.


Immunostimulatory properties of dendritic cells after Leishmania donovani infection using an in vitro model of liver microenvironment.

Donaghy L, Cabillic F, Corlu A, Rostan O, Toutirais O, Guguen-Guillouzo C, Guiguen C, Gangneux JP.

PLoS Negl Trop Dis. 2010 Jun 8;4(6):e703. doi: 10.1371/journal.pntd.0000703.


Differential toxicity of heterocyclic aromatic amines and their mixture in metabolically competent HepaRG cells.

Dumont J, Jossé R, Lambert C, Anthérieu S, Le Hegarat L, Aninat C, Robin MA, Guguen-Guillouzo C, Guillouzo A.

Toxicol Appl Pharmacol. 2010 Jun 1;245(2):256-63. doi: 10.1016/j.taap.2010.03.008. Epub 2010 Mar 20.


Reperfusion stress induced during intermittent selective clamping accelerates rat liver regeneration through JNK pathway.

Duval H, Mbatchi SF, Grandadam S, Legendre C, Loyer P, Ribault C, Piquet-Pellorce C, Guguen-Guillouzo C, Boudjema K, Corlu A.

J Hepatol. 2010 Apr;52(4):560-9. doi: 10.1016/j.jhep.2010.01.013. Epub 2010 Feb 13.


The application of 3D micropatterning of agarose substrate for cell culture and in situ comet assays.

Mercey E, Obeïd P, Glaise D, Calvo-Muñoz ML, Guguen-Guillouzo C, Fouqué B.

Biomaterials. 2010 Apr;31(12):3156-65. doi: 10.1016/j.biomaterials.2010.01.020. Epub 2010 Feb 10.


Stable expression, activity, and inducibility of cytochromes P450 in differentiated HepaRG cells.

Anthérieu S, Chesné C, Li R, Camus S, Lahoz A, Picazo L, Turpeinen M, Tolonen A, Uusitalo J, Guguen-Guillouzo C, Guillouzo A.

Drug Metab Dispos. 2010 Mar;38(3):516-25. doi: 10.1124/dmd.109.030197. Epub 2009 Dec 17.


Cyclin-dependent kinase 1 plays a critical role in DNA replication control during rat liver regeneration.

Garnier D, Loyer P, Ribault C, Guguen-Guillouzo C, Corlu A.

Hepatology. 2009 Dec;50(6):1946-56. doi: 10.1002/hep.23225.


Stem cell-derived hepatocytes and their use in toxicology.

Guguen-Guillouzo C, Corlu A, Guillouzo A.

Toxicology. 2010 Mar 30;270(1):3-9. doi: 10.1016/j.tox.2009.09.019. Epub 2009 Oct 6. Review.


Drug-metabolising enzymes are down-regulated by hypoxia in differentiated human hepatoma HepaRG cells: HIF-1alpha involvement in CYP3A4 repression.

Legendre C, Hori T, Loyer P, Aninat C, Ishida S, Glaise D, Lucas-Clerc C, Boudjema K, Guguen-Guillouzo C, Corlu A, Morel F.

Eur J Cancer. 2009 Nov;45(16):2882-92. doi: 10.1016/j.ejca.2009.07.010. Epub 2009 Aug 18.


Synthesis and kinase inhibitory activity of novel substituted indigoids.

Beauchard A, Laborie H, Rouillard H, Lozach O, Ferandin Y, Le Guével R, Guguen-Guillouzo C, Meijer L, Besson T, Thiéry V.

Bioorg Med Chem. 2009 Sep 1;17(17):6257-63. doi: 10.1016/j.bmc.2009.07.051. Epub 2009 Jul 25.


Persistence of the hepatitis B virus covalently closed circular DNA in HepaRG human hepatocyte-like cells.

Hantz O, Parent R, Durantel D, Gripon P, Guguen-Guillouzo C, Zoulim F.

J Gen Virol. 2009 Jan;90(Pt 1):127-35. doi: 10.1099/vir.0.004861-0.


Evolving concepts in liver tissue modeling and implications for in vitro toxicology.

Guillouzo A, Guguen-Guillouzo C.

Expert Opin Drug Metab Toxicol. 2008 Oct;4(10):1279-94. doi: 10.1517/17425255.4.10.1279 . Review.


Cytotoxic evaluation of sarcodifurines A and B, two novel dihydrofuroquinolines from Sarcomelicope follicularis (Rutaceae).

Chosson E, Guguen-Guillouzo C, Glaise D, Picot L, Seguin E, Besson T.

J Enzyme Inhib Med Chem. 2008 Oct;23(5):704-7. doi: 10.1080/14756360802208111 .


Localization and quantitative analysis of antigen-antibody binding on 2D substrate using imaging NanoSIMS.

Dauphas S, Delhaye T, Lavastre O, Corlu A, Guguen-Guillouzo C, Ababou-Girard S, Geneste F.

Anal Chem. 2008 Aug 1;80(15):5958-62. doi: 10.1021/ac800602q. Epub 2008 Jun 26.


Long-term functional stability of human HepaRG hepatocytes and use for chronic toxicity and genotoxicity studies.

Jossé R, Aninat C, Glaise D, Dumont J, Fessard V, Morel F, Poul JM, Guguen-Guillouzo C, Guillouzo A.

Drug Metab Dispos. 2008 Jun;36(6):1111-8. doi: 10.1124/dmd.107.019901. Epub 2008 Mar 17.


Transdifferentiation of hepatocyte-like cells from the human hepatoma HepaRG cell line through bipotent progenitor.

Cerec V, Glaise D, Garnier D, Morosan S, Turlin B, Drenou B, Gripon P, Kremsdorf D, Guguen-Guillouzo C, Corlu A.

Hepatology. 2007 Apr;45(4):957-67.


The human hepatoma HepaRG cells: a highly differentiated model for studies of liver metabolism and toxicity of xenobiotics.

Guillouzo A, Corlu A, Aninat C, Glaise D, Morel F, Guguen-Guillouzo C.

Chem Biol Interact. 2007 May 20;168(1):66-73. Epub 2006 Dec 16. Review.


Functional expression of sinusoidal and canalicular hepatic drug transporters in the differentiated human hepatoma HepaRG cell line.

Le Vee M, Jigorel E, Glaise D, Gripon P, Guguen-Guillouzo C, Fardel O.

Eur J Pharm Sci. 2006 May;28(1-2):109-17. Epub 2006 Feb 20.


Hepatocyte iron loading capacity is associated with differentiation and repression of motility in the HepaRG cell line.

Troadec MB, Glaise D, Lamirault G, Le Cunff M, Guérin E, Le Meur N, Détivaud L, Zindy P, Leroyer P, Guisle I, Duval H, Gripon P, Théret N, Boudjema K, Guguen-Guillouzo C, Brissot P, Léger JJ, Loréal O.

Genomics. 2006 Jan;87(1):93-103. Epub 2005 Dec 1.


In vitro and ex vivo permissivity of hepatocytes for Leishmania donovani.

Gangneux JP, Lemenand O, Reinhard Y, Guiguen C, Guguen-Guillouzo C, Gripon P.

J Eukaryot Microbiol. 2005 Nov-Dec;52(6):489-91.


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