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人类乙醛脱氢酶:双硫仑的抑制机制

Human aldehyde dehydrogenase: mechanism of inhibition of disulfiram.

作者信息

Vallari R C, Pietruszko R

出版信息

Science. 1982 May 7;216(4546):637-9. doi: 10.1126/science.7071604.

Abstract

Disulfiram labeled with carbon-14 reacts specifically with human liver aldehyde dehydrogenase E1 with loss of catalytic activity and no incorporation of label. Carbon-14-labeled diethyldithiocarbamate is formed and the number of enzyme sulfhydryl groups decreases from 34 to 30 during this process. Activity is recovered by-mercaptoethanol but not by glutathione, the physiological reducing agent.

摘要

用碳 -14 标记的双硫仑与人类肝脏醛脱氢酶 E1 发生特异性反应,导致催化活性丧失且无标记物掺入。在此过程中形成了碳 -14 标记的二乙基二硫代氨基甲酸盐,并且酶的巯基数量从 34 个减少到 30 个。活性可通过β - 巯基乙醇恢复,但不能通过生理还原剂谷胱甘肽恢复。

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