Oligomycin is a macrolide antibiotic, usually used as a potent inhibitor of mitochondrial F0F1-ATPase and oxidative phosphorylation, with Ki value of 1μM for inhibition of yeast intact mitochondrial ATPase activity and 0.1μM for Triton X-100-solubilized mitochondria[1]. Oligomycin at concentration of 1.5-3μM stimulated lysosome acidification due to shunting of membrane potential[2]. Treatment with 2.5μM oligomycin dramatically reduced ATP level in MII oocytes exposure to H2O2[3]. Oligomycin A exhibited antiproliferative effect on the JARID1B high subpopulation of WM3734 cells at concentration ranging in 0.1-10μg/ml post 24-72h due to the inhibition of mitochondrial respiration[4].
作用机制
Oligomycin could bind to the c10 ring of the of the yeast mitochondrial ATP synthase thereby making contact with two neighboring molecules at a position. The carboxyl side chain of Glu59, which is essential for proton translocation, forms an H-bond with oligomycin.[5]
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