ArticleBritish journal of pharmacology2010
Disruption of cellular cholesterol transport and homeostasis as a novel mechanism of action of membrane-targeted alkylphospholipid analogues.
Article in British journal of pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 38 citations in OpenAlex.
- StarD5 Regulates Cholesterol Homeostasis to Promote Colorectal Cancer Progression and the Cancer Stem Cell Phenotype.Molecular cancer research : MCR · 2026Article
- Effect of Erufosine on Membrane Lipid Order in Breast Cancer Cell Models.Biomolecules · 2020Article
- Preclinical Characterization ofJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2019Article
- Preclinical Pharmacokinetics and Dosimetry Studies ofJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2019Article
- Quantitative ubiquitylome analysis and crosstalk with proteome/acetylome analysis identified novel pathways and targets of perifosine treatment in neuroblastoma.Translational cancer research · 2018Article
- CLR 125 Auger Electrons for the Targeted Radiotherapy of Triple-Negative Breast Cancer.Cancer biotherapy & radiopharmaceuticals · 2018Article
- Proteome and Acetylome Analysis Identifies Novel Pathways and Targets Regulated by Perifosine in Neuroblastoma.Scientific reports · 2017Article
- Article
- Therapeutic combination of radiolabeled CLR1404 with external beam radiation in head and neck cancer model systems.Radiotherapy and oncology : journal of the European Society for Therapeutic Radiology and Oncology · 2015Article
- Annexins as organizers of cholesterol- and sphingomyelin-enriched membrane microdomains in Niemann-Pick type C disease.Cellular and molecular life sciences : CMLS · 2012Review
- In vitro cytotoxicity of the novel antimyeloma agents perifosine, bortezomib and lenalidomide against different cell lines.Investigational new drugs · 2012Article
- Alterations in the homeostasis of phospholipids and cholesterol by antitumor alkylphospholipids.Lipids in health and disease · 2010Article
- Adaptive Membrane Fluidity Modulation: A Feedback Regulated Homeostatic System Hiding in Plain Sight.In vivo (Athens, Greece)Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeAlkylphospholipid (APL) analogues constitute a new class of synthetic anti-tumour agents that act directly on cell membranes. We have previously demonstrated that hexadecylphosphocholine (HePC) alters intracellular cholesterol traffic and metabolism in HepG2 cells. We now extended our studies to analyse the effects of other clinically relevant APLs, such as edelfosine, erucylphosphocholine and perifosine on intracellular cholesterol homeostasis. EXPERIMENTAL APPROACH: Using radiolabelled substrates we determined the effect of APLs on cholesterol metabolism and cholesterol traffic from the plasma membrane to the endoplasmic reticulum (ER). Protein levels and gene expression of the main proteins involved in cholesterol homeostasis were analysed by Western blot and RT-PCR respectively. Membrane raft and non-raft fractions were isolated from HepG2 cells by a detergent-free method. KEY
resultsAll APLs inhibited the transport of cholesterol from the plasma membrane to the ER, which induced a significant cholesterogenic response in HepG2 cells. This response involved an increased gene expression and higher levels of several proteins related to the biosynthesis and the receptor-mediated uptake of cholesterol. Cell exposure to the APL-representative HePC enhanced the content of cholesterol mainly in the membrane raft fractions, compared with the untreated cells. CONCLUSIONS AND IMPLICATIONS: Membrane-targeted APLs exhibited a novel and common mechanism of action, through disruption of cholesterol homeostasis, which in turn affected specific lipid microdomains of cellular membranes.
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