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The linear pentadecapeptide gramicidin A forms an ion channel in the lipid bilayer to selectively transport monovalent cations. Nevertheless, we have surprisingly found that gramicidin A directly inhibits mammalian Na+/K+-ATPase. Gramicidin A inhibited ATP hydrolysis by Na+/K+-ATPase from porcine cerebral cortex at the IC50 value of 8.1 μM, while gramicidin S was approximately fivefold less active...
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