Abstract
Pentamidine and berenil, clinical antiparasitic amidines, have been found to be potent competitive inhibitors of human spermidine/spermine acetyltransferase (SSAT), K i values were found to be 2.4 and 2 μM, respectively, with spermidine as substrate. A second enzyme of polyamine back-conversion, murine polyamine oxidase (PAO), was found to be competitively inhibited by pentamidine, with a K i of 7.6 μM when N-acetylspermine was the substrate. Berenil, on the other hand, was an extremely weak inhibitor ( K i = 120 μM). The implication of the effect of inhibition of polyamine back-conversion on the growth of mammalian parasites is discussed.
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