Background: Apicularen is a specific V-ATPase inhibitor that binds to the V O complex of the holoenzyme. Results: Apicularen binds at the interface of the V O subunits a and c. Conclusion: The binding site for apicularen is in the vicinity of those for bafilomycin and archazolid. Significance: We propose the first model of binding site arrangement for these three classes of V-ATPase inhibitors.
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