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dc.contributor.authorHABRANT, D.
dc.contributor.authorPEUZIAT, P.
dc.contributor.authorCOLOMBANI, T.
dc.contributor.authorDALLET, L.
dc.contributor.authorGEHIN, J.
dc.contributor.authorGOUDEAU, E.
dc.contributor.authorEVRARD, B.
dc.contributor.authorLAMBERT, O.
dc.contributor.authorHAUDEBOURG, T.
dc.contributor.authorPITARD, B.
dc.date.accessioned2020-09-03T07:56:17Z
dc.date.available2020-09-03T07:56:17Z
dc.date.issued2016
dc.identifier.issn0022-2623
dc.identifier.urihttps://oskar-bordeaux.fr/handle/20.500.12278/10865
dc.description.abstractEnThe intracellular delivery of nucleic acid molecules is a complex process involving several distinct steps; among these the endosomal escape appeared to be of particular importance for an efficient protein production (or inhibition) into host cells. In the present study, a new series of ionizable vectors, derived from naturally occurring aminoglycoside tobramycin, was prepared using improved synthetic procedures that allow structural variations on the linker and hydrophobic domain levels. Complexes formed between the new ionizable lipids and mRNA, DNA, or siRNA were characterized by cryo-TEM experiments and their transfection potency was evaluated using different cell types. We demonstrated that lead molecule 30, bearing a biodegradable diester linker, formed small complexes with nucleic acids and provided very high transfection efficiency with all nucleic acids and cell types tested. The obtained results suggested that the improved and "universal" delivery properties of 30 resulted from an optimized endosomal escape, through the lipid-mixing mechanism.
dc.language.isoen
dc.title.enDesign of Ionizable Lipids To Overcome the Limiting Step of Endosomal Escape: Application in the Intracellular Delivery of mRNA, DNA, and siRNA
dc.typeArticle de revue
dc.subject.halChimie/Matériaux
bordeaux.journalJournal of Medicinal Chemistry
bordeaux.page3046-3062
bordeaux.volume59
bordeaux.hal.laboratoriesInstitut de Chimie & de Biologie des Membranes & des Nano-objets (CBMN) - UMR 5248*
bordeaux.hal.laboratoriesInstitut de Chimie & de Biologie des Membranes & des Nano-objets (CBMN, UMR 5248)
bordeaux.issue7
bordeaux.institutionUniversité de Bordeaux
bordeaux.institutionBordeaux INP
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