2-Aminopurine inhibits the double-stranded RNA-dependent protein kinase both in vitro and in vivo.

Y Hu, T W Conway
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引用次数: 121

Abstract

The autophosphorylation of interferon (IFN)-induced double-stranded RNA-dependent p68 protein kinase (PKR) and phosphorylation of the alpha-subunit of the translation initiation factor eIF-2 were inhibited by 10 mM 2-aminopurine in vitro. High concentrations of ATP overcame the inhibition. Kinetic studies indicated that 2-aminopurine is a competitive inhibitor with respect to ATP, suggesting that these two molecules bind the same site on the kinase. Treatment of HeLa cells with poly(I):poly(C) stimulated PKR autophosphorylation in vivo. The stimulated activity was inhibited by 10 mM 2-aminopurine to approximately the same extent as the in vitro inhibition.

2-氨基嘌呤在体外和体内均抑制双链rna依赖性蛋白激酶。
10 mM 2-氨基嘌呤可抑制干扰素(IFN)诱导的双链rna依赖性p68蛋白激酶(PKR)的自磷酸化和翻译起始因子eIF-2 α亚基的磷酸化。高浓度的ATP克服了这种抑制作用。动力学研究表明,2-氨基嘌呤是ATP的竞争性抑制剂,这表明这两个分子结合在激酶的同一位点。poly(I)处理HeLa细胞:poly(C)在体内刺激PKR自磷酸化。10 mM 2-氨基嘌呤对刺激活性的抑制程度与体外抑制程度大致相同。
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