Conjugation of a GM3 lactone mimetic on carbon nanotubes enhances the related inhibition of melanoma-associated metastatic events.
Fiche publication
Date publication
août 2018
Journal
Organic & biomolecular chemistry
Auteurs
Membres identifiés du Cancéropôle Est :
Dr MENARD-MOYON Cécilia
Tous les auteurs :
Arosio P, Comito G, Orsini F, Lascialfari A, Chiarugi P, Ménard-Moyon C, Nativi C, Richichi B
Lien Pubmed
Résumé
GM3-ganglioside is known to be involved in melanoma proliferation. In order to modulate metastatic-related events, we have functionalized multi-walled carbon nanotubes (MWCNTs) with multiple copies of a GM3-lactone mimetic. The MWCNTs proved to guarantee the appropriate spatial arrangement of the mimetic allowing a stronger inhibition of migration and invasiveness of human melanoma (A375) cells compared to other multivalent constructs reported before. In addition, the effect of the multivalent tubular conjugate on the inhibition of specific tyrosine kinases, which are associated with the ganglioside complexes within the membrane domains, was demonstrated. Finally, the short-term fate of the conjugate was assessed, for the first time, by means of the 1H NMR relaxometry technique by exploiting the signal arising from the CNTs.
Mots clés
Antineoplastic Agents, chemistry, Biomimetic Materials, chemistry, Cell Line, Tumor, G(M3) Ganglioside, analogs & derivatives, Humans, Melanoma, pathology, Models, Molecular, Molecular Conformation, Nanotubes, Carbon, chemistry, Neoplasm Metastasis
Référence
Org Biomol Chem. 2018 08 22;16(33):6086-6095