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Glutathionyl transferase catalyzed addition of glutathione to COMC: a new hypothesis for antitumor activity.
Organic Letters ( IF 4.9 ) Pub Date : 2002 Apr 4 Hamilton, Diana S, Ding, Zhebo, Ganem, Bruce, Creighton, Donald J
Organic Letters ( IF 4.9 ) Pub Date : 2002 Apr 4 Hamilton, Diana S, Ding, Zhebo, Ganem, Bruce, Creighton, Donald J
[reaction: see text] Data are presented indicating that the potent antitumor activity of 2-crotonyloxymethyl-(4R,5R,6R)-4,5,6-trihydroxy-2-cyclohexenone (COTC) and 2-crotonyloxymethyl-2-cyclohexenone (COMC) is not likely the result of glyoxalase I inhibition, as has long been assumed. An alternative hypothesis is presented, based on the finding that COMC is a substrate for human glutathionyl transferase, which produces a transient, highly electrophilic glutathionylated 2-exomethylenecyclohexanone that can covalently modify proteins and nucleic acids.
中文翻译:
谷胱甘肽转移酶催化向COMC添加谷胱甘肽:抗肿瘤活性的新假设。
[反应:参见正文]数据表明2-巴豆酰氧基甲基-(4R,5R,6R)-4,5,6-三羟基-2-环己烯酮(COTC)和2-巴豆酰氧基甲基-2-环己烯酮具有较强的抗肿瘤活性(COMC)不太可能是乙二醛酶I抑制的结果,正如长期以来所假设的那样。基于以下发现,提出了另一种假设:COMC是人谷胱甘肽转移酶的底物,该酶产生一种瞬时的,高度亲电的谷胱甘肽化的2-exomethylcyclohexanone,可以共价修饰蛋白质和核酸。
更新日期:2017-01-31
中文翻译:
谷胱甘肽转移酶催化向COMC添加谷胱甘肽:抗肿瘤活性的新假设。
[反应:参见正文]数据表明2-巴豆酰氧基甲基-(4R,5R,6R)-4,5,6-三羟基-2-环己烯酮(COTC)和2-巴豆酰氧基甲基-2-环己烯酮具有较强的抗肿瘤活性(COMC)不太可能是乙二醛酶I抑制的结果,正如长期以来所假设的那样。基于以下发现,提出了另一种假设:COMC是人谷胱甘肽转移酶的底物,该酶产生一种瞬时的,高度亲电的谷胱甘肽化的2-exomethylcyclohexanone,可以共价修饰蛋白质和核酸。