The dual-site agonist for human M2 muscarinic receptors Iper-8-naphtalimide induces mitochondrial dysfunction in <i>Saccharomyces cerevisiae</i>.

ABSTRACT: Glioblastoma is a malignant astrocytic tumor of the brain. A significantly decrease of glioblastoma cell proliferation and survival can be achieved by activating the M2 muscarinic acetylcholine receptor (a G protein-coupled receptor, or GPCR) with two agonist molecules, the orthosteric agonist Arecaidine Propargyl Ester (APE) and the dual-steric agonist Iper-8-naphthalimide (N-8-Iper). In glioblastoma cells, these agonists caused mitochondrial damage and an altered lipid profile. To characterize the mitochondrial dysfunction induced by the muscarinic agonists, we tested APE and N-8-Iper in S. cerevisiae, a yeast model system specifically suitable to study the activity of molecules of pharmaceutical interest on mitochondria. N-8-Iper, but not APE, induced mitochondrial dysfunction in

SUBMITTER: Cirigliano A 

PROVIDER: S-EPMC12713414 | biostudies-literature | 2025

REPOSITORIES: biostudies-literature