RT Journal Article
T1 Lipid–peptide bioconjugation through pyridyl disulfide reaction chemistry and its application in cell targeting and drug delivery
A1 de la Fuente Herreruela, Diego
A1 Monnappa, Ajay K.
A1 Muñoz Úbeda, Mónica
A1 Morallón Piña, Aarón
A1 Enciso Rodríguez, Eduardo
A1 Sánchez Martín, Luis
A1 Giusti, Fabrice
A1 Natale, Paolo
A1 López-Montero, Iván
AB Background: The design of efcient drug delivery vectors requires versatile formulations able to simultaneously direct a multitude of molecular targets and to bypass the endosomal recycling pathway of cells. Liposomal-based vectors need the decoration of the lipid surface with specifc peptides to fulfll the functional requirements. The unspecifc binding of peptides to the lipid surface is often accompanied with uncontrolled formulations and thus preventing the molecular mechanisms of a successful therapy. Results: We present a simple synthesis pathway to anchor cysteine-terminal peptides to thiol-reactive lipids for ade  quate and quantitative liposomal formulations. As a proof of concept, we have synthesized two diferent lipopeptides based on (a) the truncated Fibroblast Growth Factor (tbFGF) for cell targeting and (b) the pH sensitive and fusogenic GALA peptide for endosomal scape. Conclusions: The incorporation of these two lipopeptides in the liposomal formulation improves the fbroblast cell targeting and promotes the direct delivery of cargo molecules to the cytoplasm of the cell. Keywords: Smart liposomes, Disulfde bonds, Targeting peptide, GALA, Endosomal escape.
PB BMC
SN 1477-3155
YR 2019
FD 2019
LK https://hdl.handle.net/20.500.14352/12301
UL https://hdl.handle.net/20.500.14352/12301
LA eng
NO The research leading to these results has received funding from the European Research Council under the European Union's Seventh Framework Programme (ERC grant agreement n° 338133)
NO Unión Europea. FP7
DS Docta Complutense
RD 5 abr 2025