Dualsteric Agonist for M2 Muscarinic Receptor Causes Oxidative Stress and Mitochondrial Alteration in Human Glioblastoma Cancer Stem Cells - PubMed
3 days ago
- #Mitochondrial dysfunction
- #M2 muscarinic receptor
- #Glioblastoma stem cells
- The dualsteric agonist N-8-Iper and orthosteric agonist APE activate M2 muscarinic receptors, reducing proliferation and survival in glioblastoma cells and cancer stem cells (GSCs).
- N-8-Iper induces mitochondrial alterations, increases ROS production, and causes lipid droplets accumulation in both U251 and G166 GSC lines, while APE shows similar effects only in U251 cells.
- The cytotoxic effects of both agonists are specific to cancer cells, with no impact on normal human astrocytes, highlighting N-8-Iper as a potent therapeutic candidate for glioblastoma.