• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Journal of enzyme inhibition >Competitive inhibition of Trypanosoma brucei phosphoglucose isomerase by D-arabinose-5-phosphate derivatives.
【24h】

Competitive inhibition of Trypanosoma brucei phosphoglucose isomerase by D-arabinose-5-phosphate derivatives.

机译：D-阿拉伯糖-5-磷酸酯衍生物竞争抑制布鲁氏锥虫磷酸葡萄糖异构酶。

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

We report four new strong high energy intermediate analog competitive inhibitors of fructose-6-phosphate isomerization catalyzed by purified Trypanosoma brucei phosphoglucose isomerase: D-arabinonhydroxamic acid-5-phosphate, D-arabinonate-5-phosphate, D-arabinonamide-5-phosphate and D-arabinonhydrazide-5-phosphate. For comparison, the inhibitory properties of the corresponding non-phosphorylated analogues D-arabinonhydroxamic acid, D-arabinonate, D-arabinonamide and D-arabinonhydrazide were also evaluated. D-Arabinonhydroxamic acid-5-phosphate appears as the most potent competitive inhibitor ever evaluated on a phosphoglucose isomerase with an inhibition constant value of 50 nM and a Michaelis constant over inhibition constant ratio of about 2000. Our results show that anionic high energy intermediate analogues, and more particularly D-arabinonhydroxamic acid-5-phosphate, display a weak but significant specificity for Trypanosoma brucei phosphoglucose isomerase versus yeast phosphoglucose isomerase, while neutral high energy intermediate analogues are not selective at all. This would indicate the presence of more positively charged residues in the active site for Trypanosoma brucei phosphoglucose isomerase as compared to that of yeast phosphoglucose isomerase.
机译：我们报告了纯化的锥虫布鲁氏菌磷酸葡萄糖异构酶催化的果糖6-磷酸异构化的四种新的强力高能中间体类似物竞争抑制剂：D-阿拉伯羟肟酸-5-磷酸，D-阿拉伯磺酸5-磷酸，D-阿拉伯酰胺-5-磷酸。和D-阿拉伯氨酰肼-5-磷酸酯。为了比较，还评估了相应的非磷酸化类似物D-阿拉伯糖异羟肟酸，D-阿拉伯糖酸盐，D-阿拉伯糖酰胺和D-阿拉伯糖酰肼的抑制性能。 D-阿拉伯氨基异羟肟酸-5-磷酸酯是有史以来用磷酸葡萄糖异构酶评估的最有效的竞争性抑制剂，其抑制常数为50 nM，Michaelis常数超过抑制常数约2000。我们的结果表明，阴离子高能中间体类似物，特别是D-阿拉伯氢氧肟酸5-磷酸酯，对布鲁氏锥虫磷酸葡萄糖异构酶相对于酵母磷酸葡萄糖异构酶具有弱但显着的特异性，而中性高能中间体类似物则完全没有选择性。这表明与酵母磷酸葡萄糖异构酶相比，布鲁氏锥虫磷酸葡萄糖异构酶的活性位点存在更多带正电荷的残基。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号