ArticlePharmaceutics2016
Drug Transporter Expression and Activity in Human Hepatoma HuH-7 Cells.
Article in Pharmaceutics, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 37 citations in OpenAlex.
- Cytotoxic Dihydroagarofuran Sesquiterpenoids Isolated From the Roots of Tripterygium wilfordii.Chemistry & biodiversity · 2026Article
- Dexamethasone-Mediated Regulation of CYP3A4 and UGTs in Human Hepatoma HuH-7 Cells.Fundamental & clinical pharmacology · 2026Article
- Novel emerging cell and organoid systems for the study of drug metabolism and toxicity in humans.Drug metabolism and disposition: the biological fate of chemicals · 2025Review
- Drug-Metabolizing Gene Expression Identity: Comparison Across Liver Tissues and Model Cell Lines.Biomedicines · 2025Article
- Modeling of lung-liver interaction during infection in a human fluidic organ-on-a-chip.Scientific reports · 2025Article
- Article
- Comprehensive Insights into Arecoline Hydrobromide: Pharmacology, Toxicity, and Pharmacokinetics.Medical science monitor : international medical journal of experimental and clinical research · 2024Review
- A novel differentiated HuH-7 cell model to examine bile acid metabolism, transport and cholestatic hepatotoxicity.Scientific reports · 2022Article
- Expression of Chemoresistance-Associated ABC Proteins in Hepatobiliary, Pancreatic and Gastrointestinal Cancers.Cancers · 2022Review
- Disruption of small molecule transporter systems by Transporter-Interfering Chemicals (TICs).FEBS letters · 2020Review
- Transcription factor-mediated regulation of the BCRP/Expert opinion on drug metabolism & toxicology · 2020Review
- Sorafenib Activity and Disposition in Liver Cancer Does Not Depend on Organic Cation Transporter 1.Clinical pharmacology and therapeutics · 2020Article
- Targeting liver stage malaria with metformin.JCI insight · 2019Article
- Review
- Optimization of Canalicular ABC Transporter Function in HuH-7 Cells by Modification of Culture Conditions.Drug metabolism and disposition: the biological fate of chemicals · 2019Article
- Protein expression and function of organic anion transporters in short-term and long-term cultures of Huh7 human hepatoma cells.European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences · 2019Article
- mRNA Expression and Activity of Nucleoside Transporters in Human Hepatoma HepaRG Cells.Pharmaceutics · 2018Article
- SN38-PEG-PLGA-verapamil nanoparticles inhibit proliferation and downregulate drug transporter ABCG2 gene expression in colorectal cancer cells.Progress in biomaterials · 2017Article
- Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Human hepatoma cells may represent a valuable alternative to the use of human hepatocytes for studying hepatic drug transporters, which is now a regulatory issue during drug development. In the present work, we have characterized hepatic drug transporter expression, activity and regulation in human hepatoma HuH-7 cells, in order to determine the potential relevance of these cells for drug transport assays. HuH-7 cells displayed notable multidrug resistance-associated protein (MRP) activity, presumed to reflect expression of various hepatic MRPs, including MRP2. By contrast, they failed to display functional activities of the uptake transporters sodium taurocholate co-transporting polypeptide (NTCP), organic anion-transporting polypeptides (OATPs) and organic cation transporter 1 (OCT1), and of the canalicular transporters P-glycoprotein and breast cancer resistance protein (BCRP). Concomitantly, mRNA expressions of various sinusoidal and canalicular hepatic drug transporters were not detected (NTCP, OATP1B1, organic anion transporter 2 (OAT2), OCT1 and bile salt export pump) or were found to be lower (OATP1B3, OATP2B1, multidrug and toxin extrusion protein 1, BCRP and MRP3) in hepatoma HuH-7 cells than those found in human hepatocytes, whereas other transporters such as OAT7, MRP4 and MRP5 were up-regulated. HuH-7 cells additionally exhibited farnesoid X receptor (FXR)- and nuclear factor erythroid 2-related factor 2 (Nrf2)-related up-regulation of some transporters. Such data indicate that HuH-7 cells, although expressing rather poorly some main hepatic drug transporters, may be useful for investigating interactions of drugs with MRPs, notably MRP2, and for studying FXR- or Nrf2-mediated gene regulation.
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