ArticlePloS one2011
The dynamin chemical inhibitor dynasore impairs cholesterol trafficking and sterol-sensitive genes transcription in human HeLa cells and macrophages.
Article in PloS one, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 45 citations in OpenAlex.
- Dynamin inhibitor dynasore modulates longitudinal bone growth in a hormetic manner.BMC biology · 2026Article
- Article
- Mitochondrial Fission as a Therapeutic Target for Metabolic Diseases: Insights into Antioxidant Strategies.Antioxidants (Basel, Switzerland) · 2023Review
- A caveolin-1 dependent glucose-6-phosphatase trafficking contributes to hepatic glucose production.Molecular metabolism · 2023Article
- Lipids in Pathophysiology and Development of the Membrane Lipid Therapy: New Bioactive Lipids.Membranes · 2021Review
- Dynamin Inhibitors Prevent the Establishment of the Cytomegalovirus Assembly Compartment in the Early Phase of Infection.Life (Basel, Switzerland) · 2021Article
- Eruptive xanthoma model reveals endothelial cells internalize and metabolize chylomicrons, leading to extravascular triglyceride accumulation.The Journal of clinical investigation · 2021Article
- Effects of pharmacological modulators of α-synuclein and tau aggregation and internalization.Scientific reports · 2020Article
- Luteinizing hormone regulates the phosphorylation and localization of the mitochondrial effector dynamin-related protein-1 (DRP1) and steroidogenesis in the bovine corpus luteum.FASEB journal : official publication of the Federation of American Societies for Experimental Biology · 2020Article
- Macrophage-derived myeloid differentiation protein 2 plays an essential role in ox-LDL-induced inflammation and atherosclerosis.EBioMedicine · 2020Article
- New Insights Into Targeting Membrane Lipids for Cancer Therapy.Frontiers in cell and developmental biology · 2020Review
- FTY720 induces non-canonical phosphatidylserine externalization and cell death in acute myeloid leukemia.Cell death & disease · 2019Article
- Caveolin-1 and dynamin-2 overexpression is associated with the progression of bladder cancer.Oncology letters · 2019Article
- In Vitro Gene Delivery in Retinal Pigment Epithelium Cells by Plasmid DNA-Wrapped Gold Nanoparticles.Genes · 2019Article
- Genomics of lipid-laden human hepatocyte cultures enables drug target screening for the treatment of non-alcoholic fatty liver disease.BMC medical genomics · 2018Article
- LDL Cholesterol Uptake Assay Using Live Cell Imaging Analysis with Cell Health Monitoring.Journal of visualized experiments : JoVE · 2018Article
- Article
- Lipids in the cell: organisation regulates function.Cellular and molecular life sciences : CMLS · 2018Review
- Endocytosis sustains release at photoreceptor ribbon synapses by restoring fusion competence.The Journal of general physiology · 2018Article
- Osteopontin deficiency ameliorates Alport pathology by preventing tubular metabolic deficits.JCI insight · 2018Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Intracellular transport of cholesterol contributes to the regulation of cellular cholesterol homeostasis by mechanisms that are yet poorly defined. In this study, we characterized the impact of dynasore, a recently described drug that specifically inhibits the enzymatic activity of dynamin, a GTPase regulating receptor endocytosis and cholesterol trafficking. Dynasore strongly inhibited the uptake of low-density lipoprotein (LDL) in HeLa cells, and to a lower extent in human macrophages. In both cell types, dynasore treatment led to the abnormal accumulation of LDL and free cholesterol (FC) within the endolysosomal network. The measure of cholesterol esters (CE) further showed that the delivery of regulatory cholesterol to the endoplasmic reticulum (ER) was deficient. This resulted in the inhibition of the transcriptional control of the three major sterol-sensitive genes, sterol-regulatory element binding protein 2 (SREBP-2), 3-hydroxy-3-methyl-coenzymeA reductase (HMGCoAR), and low-density lipoprotein receptor (LDLR). The sequestration of cholesterol in the endolysosomal compartment impaired both the active and passive cholesterol efflux in HMDM. Our data further illustrate the importance of membrane trafficking in cholesterol homeostasis and validate dynasore as a new pharmacological tool to study the intracellular transport of cholesterol.
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Registered trials
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.