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Development of potent tripodal G-quadruplex DNA binders and their efficient delivery to cancer cells by aptamer functionalised liposomes


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Title: Development of potent tripodal G-quadruplex DNA binders and their efficient delivery to cancer cells by aptamer functionalised liposomes
Authors : Pont, Isabel
Galiana Roselló, Cristina
Sabater Arcis, María
Bargiela Schönbrunn, Ariadna
Frías Martínez, Juan Carlos
Albelda, M. Teresa
González García, Jorge
García-España, Enrique
Keywords: GenGenesQuímica orgánicaOrganic chemistryCélulaCells
Publisher: Royal Society of Chemistry
Citation: Pont, I., Galiana Roselló, C., Sabater Arcis, M., Bargiela, A., Frías, J.C., Albelda, M.T., González García, J. & García España, E. (2023). Development of potent tripodal G-quadruplex DNA binders and their efficient delivery to cancer cells by aptamer functionalised liposomes. Organic & Biomolecular Chemistry, vol. 21 (15 dec.), pp. 1000-1007. DOI: https://doi.org/10.1039/D2OB01911F
Abstract: Two new ligands (TPB3P and TPB3Py) showing a strong stabilisation effect and good selectivity for G4 over duplex DNAs have been synthesised. The ligands hold three analogous polyamine pendant arms (TPA3P and TPA3Py) but differ in the central aromatic core, which is a triphenylbenzene moiety instead of a triphenylamine moiety. Both TPB3P and TPB3Py exhibit high cytotoxicity in MCF-7, LN229 and HeLa cancer cells in contrast to TPA-based ligands, which exhibit no significant cytotoxicity. Moreover, the most potent G4 binders have been encapsulated in liposomes and AS1411 aptamer-targeted liposomes reaching nanomolar IC50 values for the most cytotoxic systems.
Description: Este es el post-print del siguiente artículo: Pont, I., Galiana Roselló, C., Sabater Arcis, M., Bargiela, A., Frías, J.C., Albelda, M.T., González García, J. & García España, E. (2023). Development of potent tripodal G-quadruplex DNA binders and their efficient delivery to cancer cells by aptamer functionalised liposomes. Organic & Biomolecular Chemistry, vol. 21 (15 dec.), pp. 1000-1007, que se ha publicado de forma definitiva en: https://doi.org/10.1039/D2OB01911F
URI: http://hdl.handle.net/10637/14865
ISSN: 1477-0520
1477-0539 (Electrónico)
Issue Date: 15-Dec-2022
Center : Universidad Cardenal Herrera-CEU
Appears in Collections:Dpto. Ciencias Biomédicas





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