Exploring the conformational behaviour and aggregation properties of lipid-conjugated AS1411 aptamers

International Journal of Biological Macromolecules
Claudia RiccardiDaniela Montesarchio

Abstract

AS1411 is a nucleolin-binding aptamer which attracted great interest as active targeting ligand for the selective delivery of therapeutic agents to tumour cells. In this work we selected three AS1411 derivatives 5'-conjugated with lipophilic tails and studied their properties in view of their application in liposomial formulations and/or lipid coated-nanoparticles for targeted therapies. The conformational behaviour of these AS1411 analogs has been investigated in comparison with the unmodified aptamer by CD, UV, PAGE, SEC-HPLC, DLS and thioflavin T (ThT) fluorescence assays to get insight in their secondary structure and aggregation properties. This study has been performed in pseudo-physiological buffers mimicking the extra- and intracellular environments, and at different concentrations in the μM range, paying special attention to the effects of the lipophilic tail on the overall aptamer conformation. The 5'-lipidated AS1411 derivatives proved to fold into stable, parallel unimolecular G-quadruplex structures, forming large aggregates, mainly micelles, at conc. >10 μM. Preliminary bioscreenings on selected cancer cells showed that these derivatives are less cytotoxic than AS1411, but maintain a similar biological behaviour. ...Continue Reading

Citations

Dec 22, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Fadwa OdehSaid I Ismail
Mar 19, 2020·International Journal of Molecular Sciences·Claudia RiccardiDaniela Montesarchio
Jul 6, 2019·Nucleic Acids Research·Federica MocciaDaniela Montesarchio
Jun 4, 2020·International Journal of Molecular Sciences·Claudia RiccardiDaniela Montesarchio
Oct 11, 2020·Medicinal Research Reviews·Claudia RiccardiDaniela Montesarchio
Mar 7, 2021·International Journal of Molecular Sciences·Anastasia A BizyaevaElena G Zavyalova
Aug 11, 2020·Pharmacology & Therapeutics·Claudia RiccardiDaniela Montesarchio
Mar 31, 2019·Analytical Biochemistry·Amirhossein BahreyniSeyed Mohammad Taghdisi
Jun 27, 2021·Nanomedicine : Nanotechnology, Biology, and Medicine·Josué CarvalhoCarla Cruz
Aug 7, 2021·Pharmaceuticals·Jéssica Lopes-NunesCarla Cruz
Sep 4, 2021·Journal of Pharmaceutical and Biomedical Analysis·Fatima BarakatLudivine Ferey

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