Two tetravalent architectures, the glycocalix 7 and the RAFT 9, presenting four residues of a GM-3 ganglioside lactone mimetic, target the host compartment of melanoma and significantly abrogate the effect induced by cancer-associated fibroblasts (CAFs) contact + hypoxia in the motility and invasiveness of tumor cells. The data reported support the involvement of glycosphingolipids (GSLs) in hypoxia and show an interesting role played by compound 9 in targeting melanoma cells thereby interfering with melanoma progression. The unprecedented findings reported for the glycocluster 9 may contribute to the understanding of the critical and complex interactions between tumor cells and their local environment paving the way for new therapeutic agents.
Role of a Preorganized Scaffold Presenting Four Residues of a GM‑3 Lactone Mimetic on Melanoma Progression / Richichi, Barbara; Comito, Giuseppina; Renaudet, Olivier; Fiore, Michele; Marra, A.; Stecca, B.; Pasquato, L.; Chiarugi, P.; Nativi, C.. - In: ACS MEDICINAL CHEMISTRY LETTERS. - ISSN 1948-5875. - ELETTRONICO. - 7:(2016), pp. 28-33. [10.1021/acsmedchemlett.5b00283]
Role of a Preorganized Scaffold Presenting Four Residues of a GM‑3 Lactone Mimetic on Melanoma Progression
RICHICHI, BARBARA;COMITO, GIUSEPPINA;CHIARUGI, PAOLA;NATIVI, CRISTINA
2016
Abstract
Two tetravalent architectures, the glycocalix 7 and the RAFT 9, presenting four residues of a GM-3 ganglioside lactone mimetic, target the host compartment of melanoma and significantly abrogate the effect induced by cancer-associated fibroblasts (CAFs) contact + hypoxia in the motility and invasiveness of tumor cells. The data reported support the involvement of glycosphingolipids (GSLs) in hypoxia and show an interesting role played by compound 9 in targeting melanoma cells thereby interfering with melanoma progression. The unprecedented findings reported for the glycocluster 9 may contribute to the understanding of the critical and complex interactions between tumor cells and their local environment paving the way for new therapeutic agents.File | Dimensione | Formato | |
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