Lamellarin D Bioconjugates II: Synthesis and Cellular Internalization of Dendrimer- and Nuclear Location Signal-Derivatives Daniel Pla, a, b Marc Martí, a Josep Farrera-Sinfreu, a, c Daniel Pulido, b, c Andrés Francesch, d Pilar Calvo, d Carmen Cuevas, d Miriam Royo, b, c Rosa Aligué, e Fernando Albericio, a, b, ‡, * and Mercedes Álvarez, a, b, §, *
[email protected] aInstitute for Research in Biomedicine, Barcelona Science Park-University of Barcelona, Baldiri Reixac 10, E-08028 Barcelona, Spain; bCIBER-BBN Networking Centre on Bioengineering, Biomaterials and Nanomedicine. cCombinatorial Chemistry Unit - Barcelona Science Park (UQC-PCB). dPharma Mar S. A., Avda de los Reyes 1, E-28770 Colmenar Viejo, Madrid, Spain. eDepartment of Cell Biology, Faculty of Medicine, University of Barcelona, Casanova 143, E-08036 Barcelona, Spain. ‡Department of Organic Chemistry, University of Barcelona, E-08028 Barcelona; §Laboratory of Organic Chemistry, Faculty of Pharmacy, University of Barcelona, E-08028 Barcelona. * Corresponding author: MA and FA, Institute for Research in Biomedicine, Barcelona Science Park-University of Barcelona, Baldiri Reixac 10, E-08028 Barcelona, Spain Tel.: +34934037086; Fax: +34934037126. ‡ Department of Organic Chemistry, University of Barcelona, E-08028 Barcelona 1 § Laboratory of Organic Chemistry, Faculty of Pharmacy, University of Barcelona, E-08028 Barcelona RECEIVED DATE (to be automatically inserted after your manuscript is accepted if required according to the journal that you are submitting your paper to) TITLE RUNNING HEAD. Lamellarin D – NLS and DTPA conjugates. ABSTRACT: 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.