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

No abstract is available for this paper.

• Publication year

  2006

• Venue

  European Journal of Pharmaceutical Sciences

• Publication date

  2006-05-01

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.1016/J.EJPS.2006.01.004PMID 16488578
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• EXPRESSION OF CYTOCHROMES P450, CONJUGATING ENZYMES AND NUCLEAR RECEPTORS IN HUMAN HEPATOMA HepaRG CELLS

  2006cited by this paper
• Evaluation of drug-drug interaction in the hepatobiliary and renal transport of drugs.

  2005cited by this paper
• FUNCTIONAL EXPRESSION OF SINUSOIDAL DRUG TRANSPORTERS IN PRIMARY HUMAN AND RAT HEPATOCYTES

  2005cited by this paper
• Mice lacking multidrug resistance protein 3 show altered morphine pharmacokinetics and morphine-6-glucuronide antinociception.

  2005cited by this paper
• Human Hepatobiliary Transport of Organic Anions Analyzed by Quadruple-Transfected Cells

  2005cited by this paper
• Physiological, pharmacological and clinical features of the multidrug resistance protein 2.

  2005cited by this paper
• Transport mechanism and substrate specificity of human organic anion transporter 2 (hOat2 [SLC22A7])

  2005cited by this paper
• Use of human-derived liver cell lines for the detection of environmental and dietary genotoxicants; current state of knowledge.

  2004cited by this paper
• The drug efflux pump MRP2: Regulation of expression in physiopathological situations and by endogenous and exogenous compounds

  2004cited by this paper
• Pharmacological and Physiological Functions of the Polyspecific Organic Cation Transporters: OCT1, 2, and 3 (SLC22A1-3)

  2004cited by this paper
• Inhibition of human organic anion transporting polypeptide OATP 1B1 as a mechanism of drug-induced hyperbilirubinemia.

  2004cited by this paper
• Human organic anion-transporting polypeptide OATP-A (SLC21A3) acts in concert with P-glycoprotein and multidrug resistance protein 2 in the vectorial transport of Saquinavir in Hep G2 cells.

  2004cited by this paper
• Organic anion transporting polypeptides of the OATP/SLC21 family: phylogenetic classification as OATP/SLCO superfamily, new nomenclature and molecular/functional properties

  2004cited by this paper
• Applications of cytotoxicity assays and pre-lethal mechanistic assays for assessment of human hepatotoxicity potential.

  2004cited by this paper
• Impact of dimethyl sulfoxide on expression of nuclear receptors and drug-inducible cytochromes P450 in primary rat hepatocytes.

  2004cited by this paper
• The bile salt export pump: molecular properties, function and regulation

  2004cited by this paper
• Pharmacokinetics of 5 (and 6)-Carboxy-2′,7′-Dichlorofluorescein and Its Diacetate Promoiety in the Liver

  2003cited by this paper
• Bile salt transporters: molecular characterization, function, and regulation.

  2003cited by this paper
• Mammalian drug efflux transporters of the ATP binding cassette (ABC) family: an overview.

  2003cited by this paper
• Detection of the Human Organic Anion Transporters SLC21A6 (OATP2) and SLC21A8 (OATP8) in Liver and Hepatocellular Carcinoma

  2003cited by this paper
• Drug transport proteins in the liver.

  2003cited by this paper
• Organic anion‐transporting polypeptide (OATP) transporter family and drug disposition

  2003cited by this paper
• Differential regulation of multidrug resistance-associated protein 2 (MRP2) and cytochromes P450 2B1/2 and 3A1/2 in phenobarbital-treated hepatocytes.

  2002cited by this paper
• The Amino Acid Residues Asparagine 354 and Isoleucine 372 of Human Farnesoid X Receptor Confer the Receptor with High Sensitivity to Chenodeoxycholate*

  2002cited by this paper
• Transporters and xenobiotic disposition.

  2002cited by this paper
• Drug transporters: their role and importance in the selection and development of new drugs.

  2002cited by this paper
• Transcellular Transport of Organic Anions Across a Double-transfected Madin-Darby Canine Kidney II Cell Monolayer Expressing Both Human Organic Anion-transporting Polypeptide (OATP2/SLC21A6) and Multidrug Resistance-associated Protein 2 (MRP2/ABCC2)*

  2002cited by this paper
• Infection of a human hepatoma cell line by hepatitis B virus

  2002cited by this paper
• Liver Protection from Apoptosis Requires Both Blockage of Initiator Caspase Activities and Inhibition of ASK1/JNK Pathway via Glutathione S-Transferase Regulation*

  2002cited by this paper
• Farnesoid X receptor and bile salts are involved in transcriptional regulation of the gene encoding the human bile salt export pump

  2002cited by this paper
• ABC transporters and inhibitors: new targets, new agents.

  2002cited by this paper
• Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver.

  2001cited by this paper
• Molecular identification of the uptake carriers for organic cations in liver

  2001cited by this paper
• Human Bile Salt Export Pump Promoter Is Transactivated by the Farnesoid X Receptor/Bile Acid Receptor*

  2001cited by this paper
• Nuclear Receptor Response Elements Mediate Induction of Intestinal MDR1 by Rifampin*

  2001cited by this paper
• Cholestatic expression pattern of sinusoidal and canalicular organic anion transport systems in primary cultured rat hepatocytes

  2001cited by this paper
• Characterization and inhibition by a wide range of xenobiotics of organic anion excretion by primary human hepatocytes.

  2000cited by this paper
• Organic anion-transporting polypeptides mediate transport of opioid peptides across blood-brain barrier.

  2000cited by this paper
• A novel human organic anion transporting polypeptide localized to the basolateral hepatocyte membrane.

  2000cited by this paper
• P-glycoprotein expression in human, mouse, hamster and rat hepatocytes in primary culture.

  1993cited by this paper
• Persistence of liver-specific messenger RNA in cultured hepatocytes: different regulatory events for different genes

  1987cited by this paper
• The human colon carcinoma cell lines HT-29 and Caco-2: two in vitro models for the study of intestinal differentiation.

  1986cited by this paper
• A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding.

  1976cited by this paper

• Making safety decisions for a sunscreen active ingredient using next-generation risk assessment: Benzophenone-4 case study.

  2025cites this paper
• Visualization-based evaluation of short-chain PFAS effects on ABCG2 in human cell models: A preliminary study

  2025cites this paper
• Functional and Transcriptional Disruption of Hepatic ABC Transporters by Environmentally Relevant Short‐Chain Per‐ and Polyfluoroalkyl Substances (PFAS)

  2025cites this paper
• Human liver cell-based assays for the prediction of hepatic bile acid efflux transporter inhibition by drugs

  2025cites this paper
• Effects of per- and polyfluoroalkyl substances on molecular initiating events of cholestatic liver injury.

  2025cites this paper
• Improved functionality of hepatic spheroids cultured in acoustic levitation compared to existing 2D and 3D models

  2024cites this paper
• Endoplasmic reticulum transporter OAT2 regulates drug metabolism and interaction.

  2024cites this paper
• Interest of molecular networking in fundamental, clinical and forensic toxicology: A state-of-the-art review

  2024cites this paper
• Amanitin-induced variable cytotoxicity in various cell lines is mediated by the different expression levels of OATP1B3.

  2024cites this paper
• Three-Dimensional Cell Co-Culture Liver Models and Their Applications in Pharmaceutical Research

  2023cites this paper
• Hepatic Bile Acid Transporters and Drug-induced Hepatotoxicity

  2023cites this paper
• Study Models of Drug–Drug Interactions Involving P-Glycoprotein: The Potential Benefit of P-Glycoprotein Modulation at the Kidney and Intestinal Levels

  2023cites this paper
• Establishment of an in vitro cholestasis risk assessment system using two-dimensional cultured HepaRG cells and 12 bile acids.

  2023cites this paper
• New approach methodologies: A quantitative in vitro to in vivo extrapolation case study with PFASs

  2022cites this paper
• Antidotal effect of cyclosporine A against α-amanitin toxicity in CD-1 mice, at clinical relevant doses.

  2022cites this paper
• Optimisation of the HepaRG cell line model for drug toxicity studies using two different cultivation conditions: advantages and limitations

  2022cites this paper
• Inhibition of canalicular and sinusoidal taurocholate efflux by cholestatic drugs in human hepatoma HepaRG cells

  2022cites this paper
• Artemisia extracts Differ from Artemisinin Effects on Human Hepatic CYP450s 2B6 and 3A4 in vitro

  2022cites this paper
• DMSO-free highly differentiated HepaRG spheroids for chronic toxicity, liver functions and genotoxicity studies

  2021cites this paper
• The utility of endogenous glycochenodeoxycholate-3-sulfate and 4β-hydroxycholesterol to evaluate the hepatic disposition of atorvastatin in rats

  2021cites this paper
• Biliary Excretion of Arsenic by Human HepaRG Cells is Stimulated by Selenide and Mediated by the Multidrug Resistance Protein 2 (MRP2/ABCC2).

  2021cites this paper
• Active Transport of Hepatotoxic Pyrrolizidine Alkaloids in HepaRG Cells

  2021cites this paper
• Runx3 regulates iron metabolism via modulation of BMP signalling

  2021cites this paper
• From street to lab: in vitro hepatotoxicity of buphedrone, butylone and 3,4-DMMC

  2021cites this paper
• Micropatterned Coculture with 3T3-J2 Fibroblasts Enhances Hepatic Functions and Drug Screening Utility of HepaRG Cells.

  2021cites this paper
• Mechanism‐Based Experimental Models for the Evaluation of BSEP Inhibition and DILI

  2021cites this paper
• Impairment of bile acid metabolism by perfluorooctanoic acid (PFOA) and perfluorooctanesulfonic acid (PFOS) in human HepaRG hepatoma cells

  2020cites this paper
• Cellular uptake and toxicity on two distinct hepatic cell models.

  2020cites this paper
• Requirements for designing organ-on-a-chip platforms to model the pathogenesis of liver disease

  2020cites this paper
• Absorption and metabolism of 3-MCPD in hepatic and renal cell lines.

  2020cites this paper
• In Vitro and in Silico Liver Models: Current Trends, Challenges and In Vitro and in Silico Liver Models: Current Trends, Challenges and Opportunities Opportunities

  2020cites this paper
• Critical role of bile acid (BA) in the cellular entry and permissiveness of Hepatitis B virus in vitro

  2020cites this paper
• Culture density contributes to hepatic functions of fresh human hepatocytes isolated from chimeric mice with humanized livers: Novel, long-term, functional two-dimensional in vitro tool for developing new drugs

  2020cites this paper
• In Vitro and in Silico Liver Models: Current Trends, Challenges and In Vitro and in Silico Liver Models: Current Trends, Challenges and Opportunities Opportunities

  2020cites this paper
• In vitro mechanistic studies on α-amanitin and its putative antidotes

  2020cites this paper
• Pyrrolizidine Alkaloids Induce Cell Death in Human HepaRG Cells in a Structure-Dependent Manner

  2020cites this paper
• Setup and Use of HepaRG Cells in Cholestasis Research.

  2019cites this paper
• Functional Comparison of HepaRG Cells and Primary Human Hepatocytes in Sandwich and Spheroid Culture as Repeated-Exposure Models for Hepatotoxicity

  2019cites this paper
• Regulatory effect of humoral milieu on the viral DNA and surface antigen expression of hepatitis B virus (HBV) in vitro

  2019cites this paper
• Total Synthesis of the Death Cap Toxin Phalloidin: Atropoisomer Selectivity Explained by Molecular-Dynamics Simulations.

  2019cites this paper
• ZIP14 is degraded in response to manganese exposure

  2019cites this paper
• Bile salts regulate CYP7A1 expression and elicit a fibrotic response and abnormal lipid production in 3D liver microtissues.

  2019cites this paper
• Tackling drug resistance with efflux pump inhibitors: from bacteria to cancerous cells

  2019cites this paper
• Validation of in vitro methods for human cytochrome P450 enzyme induction: Outcome of a multi-laboratory study

  2019cites this paper
• Differential toxic effects of bile acid mixtures in isolated mitochondria and physiologically relevant HepaRG cells

  2019cites this paper
• Protein expression and function of organic anion transporters in short‐term and long‐term cultures of Huh7 human hepatoma cells

  2019cites this paper
• Regulatory effect of humoral milieu on the viral DNA and surface antigen expression of hepatitis B virus (HBV) in vitro

  2019cites this paper
• Drug-induced liver injury

  2019cites this paper
• Evaluation of Drug Biliary Excretion Using Sandwich-Cultured Human Hepatocytes

  2018cites this paper
• Impact of cell types and culture methods on the functionality of in vitro liver systems - A review of cell systems for hepatotoxicity assessment.

  2018cites this paper
• The utility of HepaRG cells for bioenergetic investigation and detection of drug-induced mitochondrial toxicity.

  2018cites this paper
• In vitro and in silico liver models: Current trends, challenges and opportunities.

  2018cites this paper
• Advanced In Vitro HepaRG Culture Systems for Xenobiotic Metabolism and Toxicity Characterization

  2018cites this paper
• Induction of human cytochrome P450 3A4 by the irreversible myeloperoxidase inactivator PF-06282999 is mediated by the pregnane X receptor

  2018cites this paper
• Predicting drug-induced cholestasis: preclinical models

  2018cites this paper
• Flaxseed Lignan Metabolites Modulate Hepatocellular Cholesterol Trafficking In HepaRG

  2018cites this paper
• HepaRG Cells as a Model for Hepatotoxicity Studies

  2018cites this paper
• Omics-based responses induced by bosentan in human hepatoma HepaRG cell cultures

  2018cites this paper
• Use of Liver-Derived Cell Lines for the Study of Drug-Induced Liver Injury

  2018cites this paper
• mRNA Expression and Activity of Nucleoside Transporters in Human Hepatoma HepaRG Cells

  2018cites this paper
• Coadministration of antiepileptic drugs and P-glycoprotein inhibitors of flavonoid-type

  2018cites this paper
• In vitro and in silico liver models : Current trends , challenges and opportunities 1

  2018cites this paper
• Establishing species-specific 3D liver microtissues for repeat dose toxicology and advancing in vitro to in vivo translation through computational modelling

  2018cites this paper
• Quantitative Expression of Hepatobiliary Transporters and Functional Uptake of Substrates in Hepatic Two-Dimensional Sandwich Cultures: A Comparative Evaluation of Upcyte and Primary Human Hepatocytes

  2018cites this paper
• Inhibition of SLC drug transporter activities by environmental bisphenols.

  2017cites this paper
• 3D in vitro models of liver fibrosis

  2017cites this paper
• Nature et conséquences des interactions entre transporteurs membranaires et pesticides

  2017cites this paper
• Cellular Models and In Vitro Assays for the Screening of modulators of P-gp, MRP1 and BCRP

  2017cites this paper
• D in vitro models of liver fi brosis ☆

  2017cites this paper
• Application of Evolving Computational and Biological Platforms for Chemical Safety Assessment

  2017cites this paper
• Hepatitis B Virus Infection of HepaRG Cells, HepaRG-hNTCP Cells, and Primary Human Hepatocytes.

  2017cites this paper
• Expression of organic cation transporter 1 (OCT1): unique patterns of indirect regulation by nuclear receptors and hepatospecific gene regulation

  2016cites this paper
• Therapeutic potential of Omega-3 polyunsaturated fatty acids in the treatment of hepatobiliary diseases

  2016cites this paper
• INTEGRATED REACTIVE METABOLITE STRATEGIES

  2016cites this paper
• Pharmacokinetics, Pharmacodynamics and Drug Transport and Metabolism Establishment of a Drug-Induced, Bile AcideDependent Hepatotoxicity Model Using HepaRG Cells

  2016cites this paper
• Drug Transporter Expression and Activity in Human Hepatoma HuH-7 Cells

  2016cites this paper
• In vitro metabolism of the cyanotoxin cylindrospermopsin in HepaRG cells and liver tissue fractions.

  2016cites this paper
• Novel 3D Culture Systems for Studies of Human Liver Function and Assessments of the Hepatotoxicity of Drugs and Drug Candidates.

  2016cites this paper
• Disruption of BSEP Function in HepaRG Cells Alters Bile Acid Disposition and Is a Susceptive Factor to Drug-Induced Cholestatic Injury.

  2016cites this paper
• Application of Cell Culture and Tissue Models for Assessing Drug Transport

  2016cites this paper
• Analysis of real-time mixture cytotoxicity data following repeated exposure using BK/TD models.

  2016cites this paper
• In-depth quantitative analysis and comparison of the human hepatocyte and hepatoma cell line HepG2 proteomes.

  2016cites this paper
• Establishment of a Drug-Induced, Bile Acid-Dependent Hepatotoxicity Model Using HepaRG Cells.

  2016cites this paper
• The pregnane X receptor down‐regulates organic cation transporter 1 (SLC22A1) in human hepatocytes by competing for (“squelching”) SRC‐1 coactivator

  2016cites this paper
• Enhanced hepatic-targeted delivery via oral administration using nanoliposomes functionalized with a novel DSPE–PEG–cholic acid conjugate

  2016cites this paper
• Metabolic Characterization of Cell Systems Used in In Vitro Toxicology Testing

  2016cites this paper
• The role of drug metabolism in drug discovery and development : case ospemifene

  2015cites this paper
• Microengineered Liver Tissues for Drug Testing

  2015cites this paper
• HepaRG microencapsulated spheroids in DMSO-free culture: novel culturing approaches for enhanced xenobiotic and biosynthetic metabolism

  2015cites this paper
• Quantitative PCR in the assessment of novel hepatic cell models

  2015cites this paper
• Biokinetics of chlorpromazine in primary rat and human hepatocytes and human HepaRG cells after repeated exposure.

  2015cites this paper
• Protein Kinase C-Independent Inhibition of Organic Cation Transporter 1 Activity by the Bisindolylmaleimide Ro 31-8220

  2015cites this paper
• Methoden zur Transportercharakterisierung in primären Hepatozyten

  2015cites this paper
• Improved predictive models for pre-clinical drug toxicity studies

  2015cites this paper
• Régulation de l'expression fonctionnelle de transporteurs membranaires dans des cellules hépatocytaires et pulmonaires exposées aux extraits de particules diesel

  2015influential citation
• Integrating multiple omics to unravel mechanisms of Cyclosporin A induced hepatotoxicity in vitro.

  2015cites this paper
• Critical Factors in the Assessment of Cholestatic Liver Injury In Vitro.

  2015cites this paper
• Micropatterned coculture of primary human hepatocytes and supportive cells for the study of hepatotropic pathogens

  2015cites this paper
• Interleukin 6 inhibits HBV entry through NTCP down regulation.

  2015cites this paper
• Development of 3D in vitro models for prediction of hepatic metabolism and toxicity

  2015cites this paper