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)
1)
Behera MM, Purkait S, Ghosh A, Sable MN, Sahu RN, Chhabra G. The Monocarboxylate Transporters MCT1 and MCT4 Are Highly Expressed in Glioblastoma and Crucially Implicated in the Pathobiology. Neuropathology. 2025 Mar 27. doi: 10.1111/neup.70006. Epub ahead of print. PMID: 40145253.