Through a glass, darkly? HepaRG and HepG2 cells as models of human Phase I drug metabolism

PharmVar GeneFocus: CYP2C9

(2021) Katrin Sangkuhl et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Deconvolution of Cytochrome P450 Induction Mechanisms in HepaRG Nuclear Hormone Receptor Knockout Cells

(2021) Lena C. Preiss et al.   DRUG METABOLISM AND DISPOSITION

Performance of high-throughput CometChip assay using primary human hepatocytes: a comparison of DNA damage responses with in vitro human hepatoma cell lines

(2020) Ji-Eun Seo et al.   ARCHIVES OF TOXICOLOGY

Nuclear receptor phosphorylation in xenobiotic signal transduction

(2020) Masahiko Negishi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

mRNAs, proteins and the emerging principles of gene expression control

(2020) Christopher Buccitelli et al.   NATURE REVIEWS GENETICS

In-Depth Proteome Analysis Highlights HepaRG Cells as a Versatile Cell System Surrogate for Primary Human Hepatocytes

(2019) Georg Tascher et al.   Cells

Haplotype-resolved and integrated genome analysis of the cancer cell line HepG2

(2019) Bo Zhou et al.   NUCLEIC ACIDS RESEARCH

An extensively humanised mouse model to predict pathways of drug disposition, drug/drug interactions, and to facilitate the design of clinical trials

(2019) Colin James Henderson et al.   DRUG METABOLISM AND DISPOSITION

Quantitative comparison of in vitro genotoxicity between metabolically competent HepaRG cells and HepG2 cells using the high-throughput high-content CometChip assay

(2019) Ji-Eun Seo et al.   ARCHIVES OF TOXICOLOGY

A DMSO-free hepatocyte maturation medium accelerates hepatic differentiation of HepaRG cells in vitro

(2019) Zhen-Yu Wang et al.   BIOMEDICINE & PHARMACOTHERAPY

PharmVar GeneReview: CYP2D6

(2019) Charity Nofziger et al.   CLINICAL PHARMACOLOGY & THERAPEUTICS

Managing the challenge of drug-induced liver injury: a roadmap for the development and deployment of preclinical predictive models

(2019) Richard J. Weaver et al.   NATURE REVIEWS DRUG DISCOVERY

Validation of in vitro methods for human cytochrome P450 enzyme induction: Outcome of a multi-laboratory study

(2019) Camilla Bernasconi et al.   TOXICOLOGY IN VITRO

Epigenetic sensitization of pregnane X receptor-regulated gene expression by dimethyl sulfoxide

(2019) Ying Xie et al.   TOXICOLOGY LETTERS

Critical differences in drug metabolic properties of human hepatic cellular models, including primary human hepatocytes, stem cell derived hepatocytes, and hepatoma cell lines

(2018) Alexander J. Kvist et al.   BIOCHEMICAL PHARMACOLOGY

Comparison of Drug Metabolism and Its Related Hepatotoxic Effects in HepaRG, Cryopreserved Human Hepatocytes, and HepG2 Cell Cultures

(2018) Yuichi Yokoyama et al.   BIOLOGICAL & PHARMACEUTICAL BULLETIN

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

(2018) Jian Shi et al.   Drug Metabolism and Pharmacokinetics

A Transcriptional Regulatory Network Containing Nuclear Receptors and Long Noncoding RNAs Controls Basal and Drug-Induced Expression of Cytochrome P450s in HepaRG Cells

(2018) Liming Chen et al.   MOLECULAR PHARMACOLOGY

Proteomic Comparison of Various Hepatic Cell Cultures for Preclinical Safety Pharmacology

(2018) Tracey Hurrell et al.   TOXICOLOGICAL SCIENCES

Constitutive androstane receptor 1 is constitutively bound to chromatin and ‘primed’ for transactivation in hepatocytes

(2018) Michael McMahon et al.   MOLECULAR PHARMACOLOGY

Test systems in drug discovery for hazard identification and risk assessment of human drug-induced liver injury

(2017) Richard J. Weaver et al.   Expert Opinion on Drug Metabolism & Toxicology

From the Cover: Three-Dimensional (3D) HepaRG Spheroid Model With Physiologically Relevant Xenobiotic Metabolism Competence and Hepatocyte Functionality for Liver Toxicity Screening

(2017) Sreenivasa C. Ramaiahgari et al.   TOXICOLOGICAL SCIENCES

Human Hepatic HepaRG Cells Maintain an Organotypic Phenotype with High Intrinsic CYP450 Activity/Metabolism and Significantly Outperform Standard HepG2/C3A Cells for Pharmaceutical and Therapeutic Applications

(2016) Leonard J. Nelson et al.   BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY

In-depth quantitative analysis and comparison of the human hepatocyte and hepatoma cell line HepG2 proteomes

(2016) Jacek R. Wiśniewski et al.   Journal of Proteomics

Human Upcyte Hepatocytes: Characterization of the Hepatic Phenotype and Evaluation for Acute and Long-Term Hepatotoxicity Routine Testing

(2016) Laia Tolosa et al.   TOXICOLOGICAL SCIENCES

Comparison of Liver Cell Models Using the Basel Phenotyping Cocktail

(2016) Benjamin Berger et al.   Frontiers in Pharmacology

Prediction of Drug-Induced Liver Injury in HepG2 Cells Cultured with Human Liver Microsomes

(2015) Jong Min Choi et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Comparative Proteomic Characterization of 4 Human Liver-Derived Single Cell Culture Models Reveals Significant Variation in the Capacity for Drug Disposition, Bioactivation, and Detoxication

(2015) Rowena L. C. Sison-Young et al.   TOXICOLOGICAL SCIENCES

Gene Network Analysis of Glucose Linked Signaling Pathways and Their Role in Human Hepatocellular Carcinoma Cell Growth and Survival in HuH7 and HepG2 Cell Lines

(2015) Emmanuelle Berger et al.   Biomed Research International

HepaRG culture in tethered spheroids as anin vitrothree-dimensional model for drug safety screening

(2014) Zenan Wang et al.   JOURNAL OF APPLIED TOXICOLOGY

Drug metabolizing enzyme and transporter protein profiles of hepatocytes derived from human embryonic and induced pluripotent stem cells

(2013) Maria Ulvestad et al.   BIOCHEMICAL PHARMACOLOGY

Pregnane X Receptor (PXR) at the Crossroads of Human Metabolism and Disease

(2013) Ioannis Koutsounas et al.   CURRENT DRUG METABOLISM

Proteome-wide analyses of human hepatocytes during differentiation and dedifferentiation

(2013) Cliff Rowe et al.   HEPATOLOGY

Cytochrome P450 enzymes in drug metabolism: Regulation of gene expression, enzyme activities, and impact of genetic variation

(2013) Ulrich M. Zanger et al.   PHARMACOLOGY & THERAPEUTICS

Characterization of primary human hepatocytes, HepG2 cells, and HepaRG cells at the mRNA level and CYP activity in response to inducers and their predictivity for the detection of human hepatotoxins

(2012) H. H. J. Gerets et al.   CELL BIOLOGY AND TOXICOLOGY

HepaRG human hepatic cell line utility as a surrogate for primary human hepatocytes in drug metabolism assessment in vitro

(2010) Marc Lübberstedt et al.   JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS

Stable Expression, Activity, and Inducibility of Cytochromes P450 in Differentiated HepaRG Cells

(2009) S. Antherieu et al.   DRUG METABOLISM AND DISPOSITION

Evaluation of Multiple in Vitro Systems for Assessment of CYP3A4 Induction in Drug Discovery: Human Hepatocytes, Pregnane X Receptor Reporter Gene, and Fa2N-4 and HepaRG Cells

(2009) D. F. McGinnity et al.   DRUG METABOLISM AND DISPOSITION

In Vitro and in Vivo Induction of Cytochrome P450: A Survey of the Current Practices and Recommendations: A Pharmaceutical Research and Manufacturers of America Perspective

(2009) V. Chu et al.   DRUG METABOLISM AND DISPOSITION

Functional expression, inhibition and induction of CYP enzymes in HepaRG cells

(2009) Miia Turpeinen et al.   TOXICOLOGY IN VITRO

In vitromodel for the prediction of clinical CYP3A4 induction using HepaRG cells

(2009) A. Kaneko et al.   XENOBIOTICA

Comparison of Two Immortalized Human Cell Lines to Study Nuclear Receptor-Mediated CYP3A4 Induction

(2008) S. Harmsen et al.   DRUG METABOLISM AND DISPOSITION

Long-Term Functional Stability of Human HepaRG Hepatocytes and Use for Chronic Toxicity and Genotoxicity Studies

(2008) R. Josse et al.   DRUG METABOLISM AND DISPOSITION

Evaluation of HepaRG Cells as an in Vitro Model for Human Drug Metabolism Studies

(2008) K. P. Kanebratt et al.   DRUG METABOLISM AND DISPOSITION

A novel panel of mouse models to evaluate the role of human pregnane X receptor and constitutive androstane receptor in drug response

(2008) Nico Scheer et al.   JOURNAL OF CLINICAL INVESTIGATION