对羟基苯基丙酮酸双氧化酶抑制剂筛选方法研究进展

    Progress on the assay methods of p-hydroxyphenylpyruvatedioxygenase inhibitor screening

    • 摘要: 对羟基苯基丙酮酸双氧化酶(HPPD)是植物体正常生长所必需的质体醌和生育酚生物合成路径中的关键酶,已成为当前最重要的除草剂作用靶标之一。发展快速、可靠的HPPD抑制剂筛选方法对研究小分子化合物与HPPD之间的相互作用,以及开展基于靶酶结构的新型HPPD抑制剂设计均具有重要意义。结合HPPD的结构和功能,文章从生物分析的角度分别就高效液相色谱、同位素标记、偶联法、电化学及简易筛选模型等方法在HPPD抑制剂筛选中的运用进行了总结,并对发展HPPD抑制剂的高通量筛选方法进行了展望。

       

      Abstract: p-Hydroxyphenylpyruvatedioxygenase (HPPD) is one of the most important targets for herbicide discovery,due to its key involvement in the synthetic pathway of α-tocopherol and plastoquinone which are essential for plant growth.With the development and widely application of HPPD inhibitors as herbicides,rapid and efficient methods are urgently needed for both mechanism study about HPPD and high-throughput screening of the HPPD inhibitors.Based on the structure and biological function of HPPD,the application of bioanalytical methods,such as high performance liquid chromatography (HPLC),isotope labeling,coupling method,electrochemical method and simplified screening model,in screening HPPD inhibitors were reviewed.The future development of high-throughput screening methods for HPPD inhibitors were also discussed.

       

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