An inhibitor of oxidative phosphorylation in cancer cells
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Gboxin is an inhibitor of oxidative phosphorylation in cancer cells, which have a higher mitochondrial proton gradient and pH compared with non-cancerous cells.1 It increases the mitochondrial membrane potential and reduces the oxygen consumption rate, which can be bypassed by the proton ionophore FCCP , indicating that it inhibits F0F1 ATP synthase/complex V. Gboxin decreases viability of three primary mouse glioblastoma cell lines (IC50s = ~150 nM) and three patient-derived glioblastoma cultures (IC50s = ~1 ?M) but does not affect the viability of primary mouse embryonic fibroblasts or astrocytes. It halts the cell cycle in the G1/G0 phase and induces apoptosis of primary low-passage glioblastoma cells pooled from multiple tumors.
1.Shi, Y., Lim, S.K., Liang, Q., et al.Gboxin is an oxidative phosphorylation inhibitor that targets glioblastomaNature567(7748)341-346(2019)
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