Specific inhibition of the enzymic decarboxylation of S-adenosylmethionine by methylglyoxal bis(guanylhydrazone) and related substances

摘要

pMethylglyoxal bis(guanylhydrazone) {1,1′-[(methylethanediylidene)-dinitrilo]diguanidine} is a very potent inhibitor of putrescine-activated iS/i-adenosylmethionine decarboxylases from many different mammalian tissues, including sublines of mouse L1210 leukaemia that are resistant to the drug as well as sublines that are sensitive. The inhibition of purified rat ventral prostate iS/i-adenosylmethionine decarboxylase is competitive with respect to the iS/i-adenosylmethionine substrate, and is much greater in the presence than in the absence of the activator putrescine. Inhibition by the drug depends, among other things, on the nature of the aliphatic amines that can serve as stimulators of rat prostate iS/i-adenosylmethionine decarboxylase. Effects of some congeners of methylglyoxal bis(guanylhydrazone) on the enzyme are described./p