ArticleScientific reports2016
The histone deacetylase inhibiting drug Entinostat induces lipid accumulation in differentiated HepaRG cells.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. An erratum has been issued. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 21 citations in OpenAlex.
- Metabolic and Epigenetic Mechanisms in Hepatoblastoma: Insights into Tumor Biology and Therapeutic Targets.Genes · 2024Review
- Epigenetic frontiers: miRNAs, long non-coding RNAs and nanomaterials are pioneering to cancer therapy.Epigenetics & chromatin · 2024Review
- Cell Culture Systems for Studying Hepatitis B and Hepatitis D Virus Infections.Life (Basel, Switzerland) · 2023Review
- Lipid metabolic reprogramming by hypoxia-inducible factor-1 in the hypoxic tumour microenvironment.Pflugers Archiv : European journal of physiology · 2022Review
- Lipid droplet screen in human hepatocytes identifies TRRAP as a regulator of cellular triglyceride metabolism.Clinical and translational science · 2021Article
- Lipid droplet-mediated scavenging as novel intrinsic and adaptive resistance factor against the multikinase inhibitor ponatinib.International journal of cancer · 2020Article
- Lipid droplet quantification based on iterative image processing.Journal of lipid research · 2019Article
- Targeting a phospho-STAT3-miRNAs pathway improves vesicular hepatic steatosis in an in vitro and in vivo model.Scientific reports · 2018Article
- Optimized HepaRG is a suitable cell source to generate the human liver chimeric mouse model for the chronic hepatitis B virus infection.Emerging microbes & infections · 2018Article
- Regulation of Cytosolic Sulfotransferases in Models of Human Hepatocyte Development.Drug metabolism and disposition: the biological fate of chemicals · 2018Article
- Metabolic Changes Associated With Muscle Expression of SOD1Frontiers in physiology · 2018Article
- Lipid Droplet Fusion in Mammary Epithelial Cells is Regulated by Phosphatidylethanolamine Metabolism.Journal of mammary gland biology and neoplasia · 2017Article
- A systematic assessment of chemical, genetic, and epigenetic factors influencing the activity of anticancer drug KP1019 (FFC14A).Oncotarget · 2017Article
- In-line balanced detection stimulated Raman scattering microscopy.Scientific reports · 2017Article
Corrections and comments
- Erratum issued
Authors and funding
7 authors at 4 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Dietary overload of toxic, free metabolic intermediates leads to disrupted insulin signalling and fatty liver disease. However, it was recently reported that this pathway might not be universal: depletion of histone deacetylase (HDAC) enhances insulin sensitivity alongside hepatic lipid accumulation in mice, but the mechanistic role of microscopic lipid structure in this effect remains unclear. Here we study the effect of Entinostat, a synthetic HDAC inhibitor undergoing clinical trials, on hepatic lipid metabolism in the paradigmatic HepaRG liver cell line. Specifically, we statistically quantify lipid droplet morphology at single cell level utilizing label-free microscopy, coherent anti-Stokes Raman scattering, supported by gene expression. We observe Entinostat efficiently rerouting carbohydrates and free-fatty acids into lipid droplets, upregulating lipid coat protein gene Plin4, and relocating droplets nearer to the nucleus. Our results demonstrate the power of Entinostat to promote lipid synthesis and storage, allowing reduced systemic sugar levels and sequestration of toxic metabolites within protected protein-coated droplets, suggesting a potential therapeutic strategy for diseases such as diabetes and metabolic syndrome.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.