Grijalvo, SantiagoClua, AnnaEres, MarcGargallo Gómez, RaimundoEritja i Casadellà, Ramon2021-01-112021-01-112020-12-241661-6596https://hdl.handle.net/2445/173049Two G-quadruplex forming oligonucleotides [d(TG4T)4 and d(TG6T)4] were selected as two tetramolecular quadruplex nanostructures because of their demonstrated ability to be modified with hydrophobic molecules. This allowed us to synthesize two series of G-quadruplex conjugates that differed in the number of G-tetrads, as well as in the terminal position of the lipid modification. Both solution and solid-phase syntheses were carried out to yield the corresponding lipid oligonucleotide conjugates modified at their 3′- and 5′-termini, respectively. Biophysical studies confirmed that the presence of saturated alkyl chains with different lengths did not affect the G-quadruplex integrity, but increased the stability. Next, the G-quadruplex domain was added to an 18-mer antisense oligonucleotide. Gene silencing studies confirmed the ability of such G-rich oligonucleotides to facilitate the inhibition of target Renilla luciferase without showing signs of toxicity in tumor cell lines.24 p.application/pdfengcc-by (c) Grijalvo, Santiago et al., 2020http://creativecommons.org/licenses/by/3.0/esOligonucleòtidsDicroisme circularLípidsNanoestructuresOligonucleotidesCircular dichroismLipidsNanostructuresTuning G-quadruplex nanostructures with lipids. Towards designing hybrid scaffolds for oligonucleotide deliveryinfo:eu-repo/semantics/article7055262021-01-11info:eu-repo/semantics/openAccess33374392