PHARMACOLOGY

André GUILLOUZO

Nat Rev Drug Discov. 2020;19:131-148. Managing the challenge of drug-induced liver injury: a roadmap for the development and deployment of preclinical predictive models. Weaver RJ, Blomme EA, Chadwick AE, Copple IM, Gerets HHJ, Goldring CE, Guillouzo A, Hewitt PG, Ingelman-Sundberg M, Jensen KG, Juhila S, Klingmüller U, Labbe G, Liguori MJ, Lovatt CA, Morgan P, Naisbitt DJ, Pieters RHH, Snoeys J, van de Water B, Williams DP, Park BK. PubMed

Methods Mol Biol. 2019;1981:291-312. Setup and use of HepaRG cells in cholestasis research. Guguen-Guillouzo C, Guillouzo A. PubMed

Toxicol In Vitro. 2019;58:51-59. Pro-inflammatory cytokines enhance dilatation of bile canaliculi caused by cholestatic antibiotics. Sharanek A, Burban A, Ciriaci N, Guillouzo A. PubMed

Toxicol Sci. 2019;168:474-485. Predictive value of cellular accumulation of hydrophobic bile acids as a marker of cholestatic drug potential. Burban A, Sharanek A, Humbert L, Eguether T, Guguen-Guillouzo C, Rainteau D, Guillouzo A. PubMed

Free Radic Biol Med. 2018;115:166-178. Endoplasmic reticulum stress precedes oxidative stress in antibiotic-induced cholestasis and cytotoxicity in human hepatocytes. Burban A, Sharanek A, Guguen-Guillouzo C, Guillouzo A. PubMed

Toxicol Sci. 2018;161:48-57.  A dynamic mathematical model of bile acid clearance in HepaRG cells. Kaschek D, Sharanek A, Guillouzo A, Timmer J, Weaver RJ. PubMed

Drug Metab Dispos. 2017;45:1292-1303. 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. PubMed

Toxicol Sci. 2017;157:451-464. Mechanistic insights 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. PubMed

Drug Metab Dispos. 2016;44:1780-1793. 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. PubMed

Sci Rep. 2016;6:24709. 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. PubMed

Toxicol Sci. 2015;147:573-87. Cellular accumulation and toxic effects of bile acids in cyclosporine A-treated HepaRG hepatocytes. Sharanek A, Burban A, Humbert L, Bachour-El Azzi P, Felix-Gomes N, Rainteau D, Guillouzo A. PubMed

Toxicol Sci. 2015;145:157-68. 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. PubMed

Toxicol Lett. 2015;233:172-86. Understanding the biokinetics of ibuprofen after single and repeated treatments in rat and human in vitro liver cell systems. Truisi GL, Consiglio ED, Parmentier C, Savary CC, Pomponio G, Bois F, Lauer B, Jossé R, Hewitt PG, Mueller SO, Richert L, Guillouzo A, Testai E. PubMed

Drug Metab Dispos. 2014;42:1556-66. 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. PubMed

Toxicol Sci. 2014;141:244-53. 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. PubMed

Hepatology. 2013;57:1518-29. 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. PubMed

Toxicol In Vitro. 2012;26:1278-85. Optimization of the HepaRG cell model for drug metabolism and toxicity studies. Anthérieu S, Chesné C, Li R, Guguen-Guillouzo C, Guillouzo A. PubMed

Drug Metab Dispos. 2010;38:516-25. 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. PubMed

Toxicol In Vitro. 2009;23:466-75. Reproducible chemical-induced changes in gene expression profiles in human hepatoma HepaRG cells under various experimental conditions. Lambert CB, Spire C, Renaud MP, Claude N, Guillouzo A. PubMed

Drug Metab Dispos. 2008;36:1111-8. 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. PubMed

Drug Metab Rev. 2007;39:159-234. Primary hepatocytes: current understanding of the regulation of metabolic enzymes and transporter proteins, and pharmaceutical practice for the use of hepatocytes in metabolism, enzyme induction, transporter, clearance, and hepatotoxicity studies. Hewitt NJ, Lechón MJ, Houston JB, Hallifax D, Brown HS, Maurel P, Kenna JG, Gustavsson L, Lohmann C, Skonberg C, Guillouzo A, Tuschl G, Li AP, LeCluyse E, Groothuis GM, Hengstler JG. PubMed

Chem Biol Interact. 2007;168:66-73. 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. PubMed

J Pharmacol Exp Ther. 2003;304:145-55. Blockage of multidrug resistance-associated proteins potentiates the inhibitory effects of arsenic trioxide on CYP1A1 induction by polycyclic aromatic hydrocarbons. Vernhet L, Allain N, Le Vée M, Morel F, Guillouzo A, Fardel O. PubMed

Cell Biol Toxicol. 2002;18:221-33. The drug efflux pump MRP2: regulation of expression in physiopathological situations and by endogenous and exogenous compounds. Payen L, Sparfel L, Courtois A, Vernhet L, Guillouzo A, Fardel O. PubMed

J Pharmacol Exp Ther. 2001;298:234-9. Arsenic induces expression of the multidrug resistance-associated protein 2 (MRP2) gene in primary rat and human hepatocytes. Vernhet L, Séité MP, Allain N, Guillouzo A, Fardel O. PubMed

Toxicology. 2001;156:109-17. Unaltered expression of multidrug resistance transporters in polycyclic aromatic hydrocarbon-resistant rat liver cells. Payen L, Courtois A, Langouët S, Guillouzo A, Fardel O. PubMed

Biochem Pharmacol. 2000;60:1967-75. Characterization and inhibition by a wide range of xenobiotics of organic anion excretion by primary human hepatocytes. Payen L, Courtois A, Campion JP, Guillouzo A, Fardel O. PubMed

Toxicology. 2000;153:203-19. Expression and regulation of hepatic drug and bile acid transporters. Lecureur V, Courtois A, Payen L, Verhnet L, Guillouzo A, Fardel O. PubMed

Life Sci. 1999;64:763-74. Evidence for a multidrug resistance-associated protein 1 (MRP1)-related transport system in cultured rat liver biliary epithelial cells. Courtois A, Payen L, Lagadic D, Guillouzo A, Fardel O. PubMed

Cancer Lett. 1998;126:227-33. Differential expression of the polyspecific drug transporter OCT1 in rat hepatocarcinoma cells. Lecureur V, Guillouzo A, Fardel O. PubMed

Eur J Biochem. 1997;246:186-92. Up-regulation of P-glycoprotein expression in rat liver cells by acute doxorubicin treatment. Fardel O, Lecureur V, Daval S, Corlu A, Guillouzo A. PubMed

Gen Pharmacol. 1996;27:1283-91. The P-glycoprotein multidrug transporter. Fardel O, Lecureur V, Guillouzo A. PubMed

Carcinogenesis. 1996;17:1157-60. Differential regulation of mdr genes in response to 2-acetylaminofluorene treatment in cultured rat and human hepatocytes. Lecureur V, Guillouzo A, Fardel O. PubMed

Biochem Pharmacol. 1995;49:1255-60. Rifampicin enhances anti-cancer drug accumulation and activity in multidrug-resistant cells. Fardel O, Lecureur V, Loyer P, Guillouzo A. PubMed

Eur J Biochem. 1994;219:521-8. Constitutive expression of functional P-glycoprotein in rat hepatoma cells. Fardel O, Loyer P, Lecureur V, Glaise D, Guillouzo A. PubMed

FEBS Lett. 1993;327:189-93. Regulation by dexamethasone of P-glycoprotein expression in cultured rat hepatocytes. Fardel O, Lecureur V, Guillouzo A. PubMed

Carcinogenesis. 1993;14:781-3. P-glycoprotein expression in human, mouse, hamster and rat hepatocytes in primary culture. Fardel O, Morel F, Guillouzo A. PubMed

Biochem Pharmacol. 1992;44:2259-62. Modulation of multidrug resistance gene expression in rat hepatocytes maintained under various culture conditions. Fardel O, Loyer P, Morel F, Ratanasavanh D, Guillouzo A. PubMed

Eur J Biochem. 1992;205:847-52. Overexpression of the multidrug resistance gene product in adult rat hepatocytes during primary culture. Fardel O, Ratanasavanh D, Loyer P, Ketterer B, Guillouzo A. PubMed