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尿三羧酸,一种有效的NFκB-DNA结合金属螯合抑制剂。

Aurine tricarboxylic acid, a potent metal-chelating inhibitor of NFkappaB-DNA binding.

作者信息

Sharma R K, Garg B S, Kurosaki H, Goto M, Otsuka M, Yamamoto T, Inoue J

机构信息

Department of Chemistry, University of Delhi, India.

出版信息

Bioorg Med Chem. 2000 Jul;8(7):1819-23. doi: 10.1016/s0968-0896(00)00109-7.

Abstract

The metal-interaction of aurine tricarboxylic acid (ATA) and its inhibitory effect on the DNA binding of NFkappaB were studied. Chemical speciation and spectroscopic studies have shown the strong interaction of ATA with metal ions present in the biological systems. EPR, FTIR and electronic spectral studies indicated the square planar structure of the metal-binding carboxylic and hydroxyl groups of ATA indicating the ground state 2B1g. Electrophoretic mobility shift assay using NFkappaB and 32P labeled DNA has shown that ATA was inhibitory against the DNA-NFkappaB binding at 30 microM. This activity was the strongest among the metal-chelating inhibitors of NFkappaB-DNA binding reported so far.

摘要

研究了金精三羧酸(ATA)的金属相互作用及其对NFκB与DNA结合的抑制作用。化学形态和光谱研究表明,ATA与生物系统中存在的金属离子有强烈的相互作用。电子顺磁共振(EPR)、傅里叶变换红外光谱(FTIR)和电子光谱研究表明,ATA的金属结合羧基和羟基呈平面正方形结构,表明其基态为2B1g。使用NFκB和32P标记的DNA进行的电泳迁移率变动分析表明,ATA在30微摩尔浓度时对DNA-NFκB结合具有抑制作用。在迄今为止报道的NFκB-DNA结合的金属螯合抑制剂中,这种活性是最强的。

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