ArticleDrug metabolism and pharmacokinetics2018
Comparison of protein expression between human livers and the hepatic cell lines HepG2, Hep3B, and Huh7 using SWATH and MRM-HR proteomics: Focusing on drug-metabolizing enzymes.
Article in Drug metabolism and pharmacokinetics, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers.
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Who cites it
38 citing papers in PubMed.
- Dexamethasone-Mediated Regulation of CYP3A4 and UGTs in Human Hepatoma HuH-7 Cells.Fundamental & clinical pharmacology · 2026Article
- Harnessing Proteogenomics to Advance Precision Oncology: From Melanoma and Hepatocellular Carcinoma Perspective.Current oncology reports · 2026Review
- Metabolic dysfunction-associated steatotic liver disease and steatohepatitis-associated hepatocarcinoma preclinical models.Nature reviews. Gastroenterology & hepatology · 2026Review
- Target Abundance in Pharmacological Target-Mediated Drug Disposition (TMDD) for Small Molecules - A Proteomics Approach.The AAPS journal · 2026Article
- Comparative Proteomics of Hepatocytes And Hepatic Cell Lines Using Swath-MS Reveals Significant Variations In Proteins Involved In Energy, Lipid, And Xenobiotic Metabolism.Current drug metabolism · 2026Article
- Pt-Au Nanoparticles in Combination with Near-Infrared-Based Hyperthermia Increase the Temperature and Impact on the Viability and Immune Phenotype of Human Hepatocellular Carcinoma Cells.International journal of molecular sciences · 2025Article
- Bread crust extract is a novel activator of aryl hydrocarbon receptor and modulator of NRF2 and NFκB in HepG2 and HCT 116 cells.Current research in food science · 2025Article
- Comparison of the Proteome of Huh7 Cells Transfected with Hepatitis B Virus Subgenotype A1, with or without G1862T.Current issues in molecular biology · 2024Article
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- Three-Dimensional Hepatocyte Spheroids: Model for Assessing Chemotherapy in Hepatocellular Carcinoma.Biomedicines · 2024Article
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- Novel Independent Trans- and Cis-Genetic Variants Associated with CYP2D6 Expression and Activity in Human Livers.Drug metabolism and disposition: the biological fate of chemicals · 2024Article
- Distinct functional neutrophil phenotypes in sepsis patients correlate with disease severity.Frontiers in immunology · 2024Article
- Tigecycline causes loss of cell viability mediated by mitochondrial OXPHOS and RAC1 in hepatocellular carcinoma cells.Journal of translational medicine · 2023Article
- Long-term cell fate and functional maintenance of human hepatocyte through stepwise culture configuration.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2023Article
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- Coordination of AMPK and YAP byInternational journal of molecular sciences · 2022Article
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- Circular dorsal ruffles disturb the growth factor-induced PI3K-AKT pathway in hepatocellular carcinoma Hep3B cells.Cell communication and signaling : CCS · 2022Article
- Quantitative Proteomics in Translational Absorption, Distribution, Metabolism, and Excretion and Precision Medicine.Pharmacological reviews · 2022Review
Corrections and comments
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Authors and funding
5 authors.
Funding
Abstract
Human hepatic cell lines are widely used as an in vitro model for the study of drug metabolism and liver toxicity. However, the validity of this model is still a subject of debate because the expressions of various proteins in the cell lines, including drug-metabolizing enzymes (DMEs), can differ significantly from those in human livers. In the present study, we first conducted an untargeted proteomics analysis of the microsomes of the cell lines HepG2, Hep3B, and Huh7, and compared them to human livers using a sequential window acquisition of all theoretical mass spectra (SWATH) method. Furthermore, high-resolution multiple reaction monitoring (MRM-HR), a targeted proteomic approach, was utilized to compare the expressions of pre-selected DMEs between human livers and the cell lines. In general, the SWATH quantifications were in good agreement with the MRM-HR analysis. Over 3000 protein groups were quantified in the cells and human livers, and the proteome profiles of human livers significantly differed from the cell lines. Among the 101 DMEs quantified with MRM-HR, most were expressed at substantially lower levels in the cell lines. Thus, appropriate caution must be exercised when using these cell lines for the study of hepatic drug metabolism and toxicity.
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