Cancers, Vol. 11, Pages 359: The Small Molecule Ephrin Receptor Inhibitor, GLPG1790, Reduces Renewal Capabilities of Cancer Stem Cells, Showing Anti-Tumour Efficacy on Preclinical Glioblastoma Models
Cancers, Vol. 11, Pages 359: The Small Molecule Ephrin Receptor Inhibitor, GLPG1790, Reduces Renewal Capabilities of Cancer Stem Cells, Showing Anti-Tumour Efficacy on Preclinical Glioblastoma Models
Cancers doi: 10.3390/cancers11030359
Authors:
Giovanni Luca Gravina
Andrea Mancini
Alessandro Colapietro
Simona Delle Monache
Roberta Sferra
Flora Vitale
Loredana Cristiano
Stefano Martellucci
Francesco Marampon
Vincenzo Mattei
Filip Beirinckx
Philippe Pujuguet
Laurent Saniere
Giocondo Lorenzon
Ellen van der Aar
Claudio Festuccia
Therapies against glioblastoma (GBM) show a high percentage of failure associated with the survival of glioma stem cells (GSCs) that repopulate treated tumours. Forced differentiation of GSCs is a promising new approach in cancer treatment. Erythropoietin-producing hepatocellular (Eph) receptors drive tumourigenicity and stemness in GBM. We tested GLPG1790, a first small molecule with inhibition activity versus inhibitor of various Eph receptor kinases, in preclinical GBM models using in vitro and in vivo assays. GLPG1790 rapidly and persistently inhibited Ephrin-A1-mediated phosphorylation of Tyr588 and Ser897, completely blocking EphA2 receptor signalling. Similarly, this compound blocks the ephrin B2-mediated EphA3 and EphB4 tyrosine phosphorylation. This resulted in anti-glioma effects. GLPG1790 down-modulated the expression of mesenchymal markers CD44, Sox2, nestin, octamer-binding transcription factor 3/4 (Oct3...
Source: Cancers - Category: Cancer & Oncology Authors: Giovanni Luca Gravina Andrea Mancini Alessandro Colapietro Simona Delle Monache Roberta Sferra Flora Vitale Loredana Cristiano Stefano Martellucci Francesco Marampon Vincenzo Mattei Filip Beirinckx Philippe Pujuguet Laurent Saniere Giocondo Lorenzon Ellen Tags: Article Source Type: research
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