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Plasma membrane lipid bilayer is druggable: Selective delivery of gemcitabine-squalene nano-medicine to cancer cells
F. Lirussi, K. Pyrshev, S. Yesylevskyy, T. Rivel, T. Lopez, E. Coppens, S. Mura, P. Couvreur, C. Ramseyer
Jazyk angličtina Země Nizozemsko
Typ dokumentu časopisecké články
- MeSH
- buněčná membrána metabolismus MeSH
- gemcitabin MeSH
- lipidové dvojvrstvy metabolismus MeSH
- nádory * metabolismus MeSH
- prekurzory léčiv * MeSH
- skvalen metabolismus MeSH
- Publikační typ
- časopisecké články MeSH
Up to now the lipid bilayers were rarely considered as targets in cancer therapy despite pronounced differences in lipid composition between plasma membranes of benign and malignant cells. In this study we demonstrate that the lipid bilayer of the plasma membrane is druggable and suitable for facilitating selective delivery of amphiphilic gemcitabine-squalene nanomedicines to cancer cells. Data from radioactive assays, fluorescent membrane probes and molecular dynamics simulations provide evidence of selective accumulation of gemcitabine-squalene in the plasma membranes with disrupted lipid asymmetry and its subsequent preferential uptake by malignant cells. This causes pronounced cytotoxicity on cancer cells in comparison to their benign counterparts originating from the same tissue.
Receptor AI Inc 20 22 Wenlock Road London N1 7GU United Kingdom
UFR des Sciences de Santé Université Bourgogne Franche Comté F 25000 Besançon France
UMR 1231 Lipides Nutrition Cancer INSERM F 21000 Dijon France
Université Paris Saclay CNRS Institut Galien Paris Saclay 92296 Châtenay Malabry France
Citace poskytuje Crossref.org
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- $a Lirussi, Frédéric $u UMR 1231, Lipides Nutrition Cancer, INSERM, F-21000 Dijon, France; UFR des Sciences de Santé, Université Bourgogne Franche-Comté, F-25000 Besançon, France; Plateforme PACE, Laboratoire de Pharmacologie-Toxicologie, Centre Hospitalo-Universitaire Besançon, F-25000 Besançon, France. Electronic address: frederic.lirussi@u-bourgogne.fr
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- $a Up to now the lipid bilayers were rarely considered as targets in cancer therapy despite pronounced differences in lipid composition between plasma membranes of benign and malignant cells. In this study we demonstrate that the lipid bilayer of the plasma membrane is druggable and suitable for facilitating selective delivery of amphiphilic gemcitabine-squalene nanomedicines to cancer cells. Data from radioactive assays, fluorescent membrane probes and molecular dynamics simulations provide evidence of selective accumulation of gemcitabine-squalene in the plasma membranes with disrupted lipid asymmetry and its subsequent preferential uptake by malignant cells. This causes pronounced cytotoxicity on cancer cells in comparison to their benign counterparts originating from the same tissue.
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- $a Pyrshev, Kyrylo $u UFR des Sciences de Santé, Université Bourgogne Franche-Comté, F-25000 Besançon, France; Department of Physics of Biological Systems, Institute of Physics of the National Academy of Sciences of Ukraine, 46 Nauky ave, 03028 Kyiv, Ukraine; Department of Integrative Biology and Pharmacology, The University of Texas Health Science Center at Houston, 6431 Fannin St., Houston, TX 77030, USA; Department of Neurochemistry, Palladin Institute of Biochemistry of the NAS of Ukraine, 9 Leontovycha str., 01601 Kyiv, Ukraine
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