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Título: | Lamellarin D bioconjugates II: Synthesis and cellular internalization of dendrimer and nuclear location signal derivatives |
Autor: | Pla, Daniel; Martí, Marc; Farrera-Sinfreu, Josep; Pulido, Daniel; Francesch, Andrés; Calvo, Pilar; Cuevas, Carmen; Royo, Miriam CSIC ORCID ; Aligué, Rosa; Albericio, Fernando CSIC ORCID; Alvarez, Mercedes | Palabras clave: | Lamellarin D Peptides |
Fecha de publicación: | jun-2009 | Editor: | American Chemical Society | Citación: | Bioconjugate Chemistry 20 (6): 1112–1121 (2009) | Resumen: | The design and synthesis of Lamellarin D conjugates with a nuclear localization signal peptide and a poly(ethylene glycol)-based dendrimer are described. Conjugates 1-4 were obtained in 8-84% overall yields from the corresponding protected Lamellarin D. Conjugates 1 and 4 are 1.4- to 3.3-fold more cytotoxic than the parent compound against three human tumor cell lines (MDA-MB-231 breast, A-549 lung, and HT-29 colon). Besides, conjugates 3 and 4 showed a decrease in activity potency in BJ skin fibroblasts, a normal cell culture. Cellular internalization was analyzed, and a nuclear distribution pattern was observed for 4, which contains a nuclear localization signaling sequence. | Versión del editor: | https://doi.org/10.1021/bc800504t | URI: | http://hdl.handle.net/10261/346184 | DOI: | 10.1021/bc800504t | ISSN: | 10431802 |
Aparece en las colecciones: | (IQAC) Artículos |
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BioconjChem_2009.pdf | Artículo principal | 644,64 kB | Adobe PDF | Visualizar/Abrir |
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