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Título

Trehalose- and glucose-derived glycoamphiphiles: Small-molecule and nanoparticle toll-like receptor 4 (TLR4) modulators

Autor Rodríguez Lavado, J.; Sestito, Stefania E.; Cighetti, Roberto; Aguilar Moncayo, Eva M.; Oblak, Alja; Lainšček, Duško; Jiménez Blanco, José L.; García-Fernández, José Manuel; Ortiz-Mellet, Carmen; Jerala, Roman; Calabrese, Valentina; Peri, Francesco
Palabras clave TLR4
MD-2
CD14
Lipid A
LPS
Trehalose
Glucose
Glycolipids
Medicinal chemistry
Drug development
Gold nanoparticles
HEK cells
in vivo activity
Fecha de publicación 2014
EditorAmerican Chemical Society
Citación Journal of Medicinal Chemistry, 57(21): 9105-9123 (2014)
ResumenAn increasing number of pathologies have been linked to Toll-like receptor 4 (TLR4) activation and signaling, therefore new hit and lead compounds targeting this receptor activation process are urgently needed. We report on the synthesis and biological properties of glycolipids based on glucose and trehalose scaffolds which potently inhibit TLR4 activation and signaling in vitro and in vivo. Structure-activity relationship studies on these compounds indicate that the presence of fatty ester chains in the molecule is a primary prerequisite for biological activity and point to facial amphiphilicity as a preferred architecture for TLR4 antagonism. The cationic glycolipids here presented can be considered as new lead compounds for the development of drugs targeting TLR4 activation and signaling in infectious, inflammatory, and autoimmune diseases. Interestingly, the biological activity of the best drug candidate was retained after adsorption at the surface of colloidal gold nanoparticles, broadening the options for clinical development.
Versión del editorhttp://dx.doi.org/10.1021/jm501182w
URI http://hdl.handle.net/10261/112376
DOI10.1021/jm501182w
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