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二苯基磷酰基乙酰胆碱酯酶的再活化与老化

Reactivation and aging of diphenyl phosphoryl acetylcholinesterase.

作者信息

Maglothin J A, Wins P, Wilson I B

出版信息

Biochim Biophys Acta. 1975 Oct 22;403(2):370-87. doi: 10.1016/0005-2744(75)90066-2.

DOI:10.1016/0005-2744(75)90066-2
PMID:241402
Abstract

Acetylcholinesterase (acetylcholine hydrolase, EC 3.1.1.7) is readily in hibited by 10(-5) M diphenylphosphorochloridate even though the inhibitor hydrolyzes in a few seconds. The fluoridate is a much weaker inhibitor. The inhibited enzyme, diphenyl phosphoryl enzyme spontaneously recovers only about 50% of its activity with a half time of about 17 min at pH 7.0 and 6 min at pH 8.0. The fact that only 50% of the original activity returns is due to aging. The rates of reactivation and aging can be very greatly increased by a few percent of an organic solvent. Depending on the solvent even 1% may increase the rates by a factor of 5 or 6. The highest increase in rate was 70-fold. Quaternary NH+4 also increases the rates. Organic solvents and NH+4 also accelerate the reactivation of the much more stable diethyl phosphoryl enzyme derivative.

摘要

乙酰胆碱酯酶(乙酰胆碱水解酶,EC 3.1.1.7)很容易被10⁻⁵M的二苯基磷酰氯抑制,尽管该抑制剂在几秒钟内就会水解。氟化物是一种较弱的抑制剂。被抑制的酶,即二苯基磷酰酶,在pH 7.0时约17分钟、pH 8.0时约6分钟的半衰期下,自发恢复的活性仅约为其原始活性的50%。只有50%的原始活性恢复这一事实是由于老化。加入百分之几的有机溶剂可极大地提高再活化和老化的速率。根据溶剂的不同,即使是1%也可能使速率提高5到6倍。速率的最高提高倍数为70倍。季铵离子NH₄⁺也能提高速率。有机溶剂和NH₄⁺还能加速更稳定的二乙基磷酰酶衍生物的再活化。

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Reactivation and aging of diphenyl phosphoryl acetylcholinesterase.二苯基磷酰基乙酰胆碱酯酶的再活化与老化
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引用本文的文献

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Kinetics of protein modification, and/or enzyme inactivation, reactions by an unstable modifying agent.不稳定修饰剂引发的蛋白质修饰和/或酶失活反应的动力学
Biochem J. 1987 Sep 15;246(3):803-5. doi: 10.1042/bj2460803.
4
Formation of an unstable covalent intermediate during the inhibition of electric-eel acetylcholinesterase with 1,3,2-dioxaphosphorinane 2-oxides.用1,3,2-二氧磷杂环己烷-2-氧化物抑制电鳗乙酰胆碱酯酶过程中不稳定共价中间体的形成。
Biochem J. 1979 Mar 1;177(3):781-90. doi: 10.1042/bj1770781.