乙醇胺 O-硫酸盐在体外和体内对大鼠脑 4-氨基丁酸转氨酶的活性位点定向不可逆抑制作用。
Active-site-directed irreversible inhibition of rat brain 4-aminobutyrate aminotransferase by ethanolamine O-sulphate in vitro and in vivo.
作者信息
Fowler L J, John R A
出版信息
Biochem J. 1972 Nov;130(2):569-73. doi: 10.1042/bj1300569.
Abstract
- Partially purified preparations of rat brain 4-aminobutyrate aminotransferase were inhibited in a time-dependent manner by ethanolamine O-sulphate. The inhibition was not reversed by dialysis. 2. The inhibitor formed an initial reversible complex with the enzyme (K(i)=4.4x10(-4)m) and the rate of inactivation followed pseudo-first-order kinetics (k=7.15x10(-4)s(-1)). The inclusion of 4-aminobutyrate markedly slowed the rate of inactivation. 3. Ethanolamine O-sulphate did not inhibit glutamate decarboxylase, alanine aminotransferase or aspartate aminotransferase. 4. Intracisternal injection of ethanolamine O-sulphate into rats led to rapid inactivation of 4-aminobutyrate aminotransferase in vivo.
摘要
- 大鼠脑4-氨基丁酸转氨酶的部分纯化制剂被乙醇胺O-硫酸盐以时间依赖性方式抑制。透析不能逆转这种抑制作用。2. 抑制剂与酶形成初始可逆复合物（K(i)=4.4×10⁻⁴m），失活速率遵循假一级动力学（k=7.15×10⁻⁴s⁻¹）。加入4-氨基丁酸显著减慢了失活速率。3. 乙醇胺O-硫酸盐不抑制谷氨酸脱羧酶、丙氨酸转氨酶或天冬氨酸转氨酶。4. 向大鼠脑池内注射乙醇胺O-硫酸盐导致体内4-氨基丁酸转氨酶迅速失活。
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本文引用的文献
1
Protein measurement with the Folin phenol reagent.使用福林酚试剂进行蛋白质测定。
J Biol Chem. 1951 Nov;193(1):265-75.
2
Infrared studies on sulphate esters. III. O-Sulphate esters of alcohols, amino alcohols and hydroxylated amino acids.硫酸酯的红外光谱研究。III. 醇、氨基醇和羟基化氨基酸的O-硫酸酯
Biochim Biophys Acta. 1961 Sep 30;52:413-9. doi: 10.1016/0006-3002(61)90397-3.
3
THE ENZYMIC MEASUREMENT OF GAMMA-AMINOBUTYRIC-ALPHA-OXOGLUTARIC TRANSAMINASE.γ-氨基丁酸-α-酮戊二酸转氨酶的酶法测定
J Neurochem. 1965 Feb;12:93-101. doi: 10.1111/j.1471-4159.1965.tb11944.x.
4
Esters of methanesulfonic acid as irreversible inhibitors of acetylcholinesterase.甲磺酸酯作为乙酰胆碱酯酶的不可逆抑制剂
J Biol Chem. 1962 Oct;237:3245-9.
5
Some properties of L-glutamic decarboxylase in mouse brain.小鼠脑中L-谷氨酸脱羧酶的一些特性
Biochem Pharmacol. 1963 Feb;12:113-34. doi: 10.1016/0006-2952(63)90177-1.
6
7
Studies on the GABA pathway. I. The inhibition of gamma-aminobutyric acid-alpha-ketoglutaric acid transaminase in vitro and in vivo by U-7524 (amino-oxyacetic acid).γ-氨基丁酸通路的研究。I. U-7524（氨氧基乙酸）对体外和体内γ-氨基丁酸-α-酮戊二酸转氨酶的抑制作用。
Biochem Pharmacol. 1961 Feb;5:323-31. doi: 10.1016/0006-2952(61)90023-5.
8
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J Biol Chem. 1959 Apr;234(4):922-5.
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10
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