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http://hdl.handle.net/10637/14865Development of potent tripodal G-quadruplex DNA binders and their efficient delivery to cancer cells by aptamer functionalised liposomes
| 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: | Gen; Genes; Química orgánica; Organic chemistry; Célula; Cells |
| 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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