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Lamellarin D bioconjugates II: synthesis and cellular internalization of dendrimer and nuclear location signal derivatives

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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, 4 showed a decrease in activity potency in BJ skin fibroblasts, a normal cell culture. Cellular internalization was analyzed and nuclear distribution pattern was observed for 4, which contains a nuclear localization signalling sequence.

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PLA QUERAL, Daniel, MARTÍ, Marc, FARRERA SINFREU, Josep maria, PULIDO, Daniel, FRANCESCH, Andrés, CALVO, Pilar, CUEVAS, Carmen, ROYO EXPÓSITO, Miriam, ALIGUÉ I ALEMANY, Rosa maria, ALBERICIO PALOMERA, Fernando, ÁLVAREZ DOMINGO, Mercedes. Lamellarin D bioconjugates II: synthesis and cellular internalization of dendrimer and nuclear location signal derivatives. _Bioconjugate Chemistry_. 2009. Vol. 20, núm. 6, pàgs. 1112-1121. [consulta: 23 de gener de 2026]. ISSN: 1043-1802. [Disponible a: https://hdl.handle.net/2445/56025]

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