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Please use this identifier to cite or link to this item: https://hdl.handle.net/2445/173049
Tuning G-quadruplex nanostructures with lipids. Towards designing hybrid scaffolds for oligonucleotide delivery
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Two 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.
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GRIJALVO, Santiago, et al. Tuning G-quadruplex nanostructures with lipids. Towards designing hybrid scaffolds for oligonucleotide delivery. International Journal of Molecular Sciences. 2020. Vol. 22, num. 121. ISSN 1661-6596. [consulted: 17 of August of 2026]. Available at: https://hdl.handle.net/2445/173049