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甲基乙二醛双(脒腙)及相关物质对S-腺苷甲硫氨酸酶促脱羧作用的特异性抑制

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

作者信息

Corti A, Dave C, Williams-Ashman H G, Mihich E, Schenone A

出版信息

Biochem J. 1974 May;139(2):351-7. doi: 10.1042/bj1390351.

Abstract

Methylglyoxal bis(guanylhydrazone) {1,1'-[(methylethanediylidene)-dinitrilo]diguanidine} is a very potent inhibitor of putrescine-activated S-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 S-adenosylmethionine decarboxylase is competitive with respect to the S-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 S-adenosylmethionine decarboxylase. Effects of some congeners of methylglyoxal bis(guanylhydrazone) on the enzyme are described.

摘要

甲基乙二醛双(胍腙){1,1'-[(甲基亚乙基)-二氮基]二胍}是一种非常有效的抑制剂,可抑制来自许多不同哺乳动物组织的腐胺激活的S-腺苷甲硫氨酸脱羧酶,包括对该药物耐药的小鼠L1210白血病亚系以及敏感亚系。纯化的大鼠腹侧前列腺S-腺苷甲硫氨酸脱羧酶的抑制作用相对于S-腺苷甲硫氨酸底物具有竞争性,并且在有激活剂腐胺存在时比不存在时要强得多。该药物的抑制作用尤其取决于可作为大鼠前列腺S-腺苷甲硫氨酸脱羧酶刺激剂的脂肪族胺的性质。描述了甲基乙二醛双(胍腙)的一些同系物对该酶的影响。

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