Fig. 1: Inhibition of F1Fo ATP synthase.
From: Bedaquiline inhibits the yeast and human mitochondrial ATP synthases
a Inhibition of the ATPase activity of the purified yeast ATP synthase reconstituted in bicelles. Inhibition of the ATPase activity by oligomycin A (EC50: 107 ± 1.1 nM, (n = 3)) and BDQ (EC50: 27 ± 2.5 nM, (n = 3)) b Inhibition of the ATP synthase activity by bedaquiline of yeast mitochondria (IC50: 1.1 ± 0.05 µM (n = 3)) and human mitoplasts (IC50: 0.66 ± 0.05 µM (n = 5)). c, d Mitochondrial membrane potential. c Human mitoplasts and d yeast mitochondria. e Structure of oligomycin A, B, and C. f Structure of bedaquiline. Membrane potential was measured by fluorescence quenching of Rhodamine 123 (excitation at 488 nm and emission at 525 nm). Rhodamine 123 (1.0 μM), mitochondria or mitoplasts (150 μg, mito), ethanol (68 mM, ETOH), glutamate/malate (5.0 mM/2.5 mM), NaCN (0.5 mM).
