Cellular Accumulation and Toxic Effects of Bile Acids in Cyclosporine A-Treated HepaRG Hepatocytes.

No abstract is available for this paper.

• Publication year

  2015

• Venue

  Toxicological Sciences

• Publication date

  2015-10-01

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.1093/toxsci/kfv155PMID 26198044
• 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.

• Bile acid-induced necrosis in primary human hepatocytes and in patients with obstructive cholestasis.

  2015cited by this paper
• Comparative Localization and Functional Activity of the Main Hepatobiliary Transporters in HepaRG Cells and Primary Human Hepatocytes.

  2015cited by this paper
• Potency of individual bile acids to regulate bile acid synthesis and transport genes in primary human hepatocyte cultures.

  2014cited by this paper
• Different dose-dependent mechanisms are involved in early cyclosporine a-induced cholestatic effects in hepaRG cells.

  2014influential reference
• A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.

  2013cited by this paper
• Cytochromes P450: Roles in Diseases*

  2013cited by this paper
• Phase 1 and Phase 2 Drug Metabolism and Bile Acid Production of HepaRG Cells in a Bioartificial Liver in Absence of Dimethyl Sulfoxide

  2013cited by this paper
• Efficacy and safety of the farnesoid X receptor agonist obeticholic acid in patients with type 2 diabetes and nonalcoholic fatty liver disease.

  2013cited by this paper
• Oxidative stress plays a major role in chlorpromazine‐induced cholestasis in human HepaRG cells

  2013cited by this paper
• Drug-induced cholestasis.

  2013cited by this paper
• Bile formation and secretion.

  2013cited by this paper
• Interindividual Variability in Gene Expression Profiles in Human Hepatocytes and Comparison with HepaRG Cells

  2012cited by this paper
• Cyclosporine A- and Tacrolimus-Mediated Inhibition of CYP3A4 and CYP3A5 In Vitro

  2012cited by this paper
• Endogenous bile acid disposition in rat and human sandwich-cultured hepatocytes.

  2012cited by this paper
• Bile acid profiling in human biological samples: comparison of extraction procedures and application to normal and cholestatic patients.

  2012cited by this paper
• The use of human hepatocytes to investigate bile acid synthesis.

  2010cited by this paper
• General review on in vitro hepatocyte models and their applications.

  2010cited by this paper
• New molecular insights into the mechanisms of cholestasis.

  2009cited by this paper
• Biochemical mechanisms in drug-induced liver injury: certainties and doubts.

  2009cited by this paper
• Lithocholic acid as a biomarker of intrahepatic cholestasis of pregnancy during ursodeoxycholic acid treatment

  2009cited by this paper
• Bile Acid sulfation: a pathway of bile acid elimination and detoxification.

  2009cited by this paper
• Bile acids: regulation of synthesis

  2009cited by this paper
• Bile acid transporters

  2009cited by this paper
• Long-Term Functional Stability of Human HepaRG Hepatocytes and Use for Chronic Toxicity and Genotoxicity Studies

  2008cited by this paper
• Transdifferentiation of hepatocyte‐like cells from the human hepatoma HepaRG cell line through bipotent progenitor

  2007cited by this paper
• The bile salt export pump

  2007cited by this paper
• Determination of the hepatocellularity number for human, dog, rabbit, rat and mouse livers from protein concentration measurements.

  2007cited by this paper
• Role of nuclear receptors in the adaptive response to bile acids and cholestasis: pathogenetic and therapeutic considerations.

  2006cited by this paper
• Determination of the hepatocellularity number for human, dog, rabbit, rat and mouse livers from protein concentration measurements

  2006cited by this paper
• EXPRESSION OF CYTOCHROMES P450, CONJUGATING ENZYMES AND NUCLEAR RECEPTORS IN HUMAN HEPATOMA HepaRG CELLS

  2006cited by this paper
• Enterohepatic transport of bile salts and genetics of cholestasis.

  2005cited by this paper
• Enterohepatic bile salt transporters in normal physiology and liver disease.

  2004cited by this paper
• Detoxification of Lithocholic Acid, A Toxic Bile Acid: Relevance to Drug Hepatotoxicity

  2004influential reference
• Steroid and bile acid conjugates are substrates of human multidrug-resistance protein (MRP) 4 (ATP-binding cassette C4).

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

  2003cited by this paper
• Feedback regulation of bile acid synthesis in primary human hepatocytes: Evidence that CDCA is the strongest inhibitor

  2003cited by this paper
• Drug-induced hepatotoxicity.

  2003cited by this paper
• An essential role for nuclear receptors SXR/PXR in detoxification of cholestatic bile acids

  2001cited by this paper
• Predominance of human versus rat phenotype in the metabolic pathways for bile acid synthesis by hybrid WIF-B9 cells.

  2001cited by this paper
• Bile acid formation in primary human hepatocytes.

  2000cited by this paper
• Bile acid synthesis in cultured human hepatocytes: support for an alternative biosynthetic pathway to cholic acid

  2000influential reference
• ATP-dependent Transport of Bile Salts by Rat Multidrug Resistance-associated Protein 3 (Mrp3)*

  2000cited by this paper
• Bile acid synthesis in primary cultures of rat and human hepatocytes

  1998cited by this paper
• Cyclosporin A-mediated cholestasis in patients with chronic hepatitis after heart transplantation.

  1996cited by this paper
• [Drug-induced cholestasis].

  1995cited by this paper
• Bile acid transporters

  1995cited by this paper
• Drug-induced hepatotoxicity.

  1995cited by this paper
• Bile acid synthesis in cultured human hepatoblastoma cells.

  1991cited by this paper
• Cyclosporin A blocks bile acid synthesis in cultured hepatocytes by specific inhibition of chenodeoxycholic acid synthesis.

  1991influential reference
• HepG2. A human hepatoblastoma cell line exhibiting defects in bile acid synthesis and conjugation.

  1986cited by this paper
• High yield preparation of isolated human adult hepatocytes by enzymatic perfusion of the liver.

  1982cited by this paper

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  2025cites this paper
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  2025cites this paper
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  2025cites this paper
• In vitro test battery for testing molecular initiating events in chemical-induced cholestasis.

  2025cites this paper
• Cell-based approaches for the mechanistic understanding of drug-induced cholestatic liver injury

  2025cites this paper
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  2024cites this paper
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  2024cites this paper
• Intestinal in vitro transport assay combined with physiologically based kinetic modeling as a tool to predict bile acid levels in vivo.

  2023cites this paper
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  2022cites this paper
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  2022cites this paper
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  2022cites this paper
• Hepatic bile acid synthesis and secretion: comparison of in vitro methods.

  2022cites this paper
• Mouse precision-cut liver slices as an ex vivo model to study drug-induced cholestasis

  2022cites this paper
• Oxidative-stress and long-term hepatotoxicity: comparative study in Upcyte human hepatocytes and hepaRG cells

  2022cites this paper
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  2021influential citation
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  2021cites this paper
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  2021cites this paper
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  2021cites this paper
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  2020cites this paper
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  2020cites this paper
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  2019cites this paper
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  2019cites this paper
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  2019cites this paper
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  2019cites this paper
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  2019cites this paper
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  2019cites this paper
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  2019cites this paper
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  2019cites this paper
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  2019cites this paper
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  2018cites this paper
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  2018cites this paper
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  2018influential citation
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  2018influential citation
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  2018cites this paper
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  2017cites this paper
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  2017influential citation
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  2017cites this paper
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  2017cites this paper
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