MCT1
High Expression in GBM:
MCT1 and MCT4 are significantly overexpressed in IDH-wildtype glioblastomas compared to IDH-mutant gliomas (grades 2–4), both at the protein (IHC) and mRNA levels.
Endothelial Proliferation Specificity:
Loss of MCT1 expression was noted in areas of endothelial proliferation within grade 4 gliomas, contrasting with its presence in non-proliferating endothelium—suggesting a specific microenvironmental regulation.
Prognostic Implications:
High MCT1/4 expression correlates with shorter overall survival when analyzing all gliomas together, although this correlation was not significant in GBM alone.
Therapeutic Insight – Syrosingopine:
Syrosingopine, a dual MCT1/4 inhibitor and old antihypertensive drug with good CNS penetration, showed dose-dependent anti-tumor effects in vitro on U87MG and LN229 glioma cell lines:
Increased cytotoxicity
Enhanced apoptosis
Reduced migration/invasion
Clinical Relevance:
MCT1/4 may serve as diagnostic immunohistochemical markers.
Syrosingopine, a dual MCT1/4 inhibitor and old antihypertensive drug with good CNS penetration, showed dose-dependent anti-tumor effects in vitro on U87MG and LN229 glioma cell lines:
Increased cytotoxicity
Enhanced apoptosis
Reduced migration/invasion
Clinical Relevance:
MCT1/4 may serve as diagnostic immunohistochemical markers.
Syrosingopine may represent a promising adjunctive therapy for GBM 1)