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大肠杆菌苯丙氨酰 - tRNA合成酶的体内抑制剂。

In vivo inhibitors of Escherichia coli phenylalanyl-tRNA synthetase.

作者信息

Santi D V, Cunnion S O, Anderson R T, Webster R W

出版信息

J Med Chem. 1979 Oct;22(10):1260-3. doi: 10.1021/jm00196a021.

DOI:10.1021/jm00196a021
PMID:390149
Abstract

N-Benzyl-D-amphetamine is a potent in vitro and in vivo inhibitor of phenylalanyl-tRNA synthetase of Escherichia coli. The concentration of this inhibitor necessary for the in vivo inhibition is approximately 100-fold greater than that necessary for inhibition of the purified enzyme. Treatment of rel+ strains of E. coli with the inhibitor results in a decreased percentage of tRNA Phe which is charged, guanosine tetraphosphate formation, cessation of RNA synthesis, and growth arrest. Evidence is presented which demonstrates that the primary and perhaps sole mode of action of N-benzyl-D-amphetamine is inhibition of phenylalanyl-tRNA synthetase.

摘要

N-苄基-D-苯丙胺是一种对大肠杆菌苯丙氨酰-tRNA合成酶具有强大体外和体内抑制作用的物质。体内抑制所需的该抑制剂浓度比抑制纯化酶所需的浓度大约高100倍。用该抑制剂处理大肠杆菌的rel+菌株会导致苯丙氨酰-tRNA负载的百分比降低、四磷酸鸟苷形成、RNA合成停止以及生长停滞。有证据表明,N-苄基-D-苯丙胺的主要作用方式(可能也是唯一作用方式)是抑制苯丙氨酰-tRNA合成酶。

相似文献

1
In vivo inhibitors of Escherichia coli phenylalanyl-tRNA synthetase.大肠杆菌苯丙氨酰 - tRNA合成酶的体内抑制剂。
J Med Chem. 1979 Oct;22(10):1260-3. doi: 10.1021/jm00196a021.
2
Phenylalanyl transfer ribonucleic acid synthetase from Escherichia coli B. Potent inhibition by analogues of N-benzyl-2-phenylethylamine.
J Med Chem. 1976 Nov;19(11):1270-5. doi: 10.1021/jm00233a002.
3
Inhibition of phenylalanyl-tRNA synthetase by aromatic guanidines and amidines.
J Med Chem. 1975 May;18(5):528-30. doi: 10.1021/jm00239a021.
4
Zinc(II)-dependent synthesis of diadenosine 5', 5"' -P(1) ,P(4) -tetraphosphate by Escherichia coli and yeast phenylalanyl transfer ribonucleic acid synthetases.锌(II)依赖型大肠杆菌和酵母苯丙氨酰转移核糖核酸合成酶合成5',5"' -P(1),P(4) -四磷酸二腺苷。
Biochemistry. 1981 Aug 4;20(16):4654-62. doi: 10.1021/bi00519a021.
5
Phenylalanyl transfer ribonucleic acid synthetase from rat liver. Analysis of phenylalanine and adenosine 5'-triphosphate binding sites and comparison to the enzyme from Escherichia coli.
J Med Chem. 1976 Nov;19(11):1276-9. doi: 10.1021/jm00233a003.
6
[Chemical modification of the complex of tRNA Phe with phenylalanyl-tRNA synthetase from Escherichia coli].[大肠杆菌苯丙氨酰 - tRNA合成酶与tRNA Phe复合物的化学修饰]
Mol Biol (Mosk). 1979 Sep-Oct;13(5):994-1000.
7
[Modification of the alpha-subunit of phenylalanyl-tRNA synthetase from E. coli MRE-600 with N-chlorambucilyl-phenylalanyl-tRNA].[用N-苯丁酸氮芥基苯丙氨酰-tRNA对大肠杆菌MRE-600苯丙氨酰-tRNA合成酶α亚基的修饰]
Biokhimiia. 1979 Mar;44(3):570-2.
8
Phenylalanyl-tRNA synthetase induced conformational change of Escherichia coli tRNA phe.苯丙氨酰 - tRNA合成酶诱导大肠杆菌苯丙氨酸tRNA的构象变化。
Biochemistry. 1979 Jun 26;18(13):2887-95. doi: 10.1021/bi00580a033.
9
[Alkylation of tRNA-Phe free and bound to phenylalanyl-tRNA synthetase with 4-(N-2-chloroethyl-N-methylamino)benzylamine].[用4-(N-2-氯乙基-N-甲基氨基)苄胺对游离的和与苯丙氨酰-tRNA合成酶结合的tRNA-苯丙氨酸进行烷基化反应]
Mol Biol (Mosk). 1981 Jan-Feb;15(1):45-53.
10
[Effect of diadenosine oligophosphates (Ap4A and Ap3A) and their phosphonate analogs on catalytic properties of phenylalanyl-tRNA synthetase from E. coli].[二腺苷寡磷酸(Ap4A和Ap3A)及其膦酸酯类似物对大肠杆菌苯丙氨酰-tRNA合成酶催化特性的影响]
Bioorg Khim. 1987 Sep;13(9):1164-9.

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Simple Secondary Amines Inhibit Growth of Gram-Negative Bacteria through Highly Selective Binding to Phenylalanyl-tRNA Synthetase.简单的仲胺通过与苯丙氨酰-tRNA 合成酶的高选择性结合来抑制革兰氏阴性菌的生长。
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2
Real-time assay for testing components of protein synthesis.实时检测蛋白质合成成分的分析方法。
Nucleic Acids Res. 2012 Jul;40(12):e88. doi: 10.1093/nar/gks232. Epub 2012 Mar 14.