新型杀菌化合物靶标识别及其靶向候选药剂设计概述  

General summary of novel fungicide target identification and itstargeted candidate design

作　　者：赵斌 陈来[1,2] 张乃楼 范志金 ZHAO Bin1,2,CHEN Lai1,2,ZHANG Nailou1,2,FAN Zhijin1,2(1. State Key Laboratory of Elemento-Organic Chemistry, College of Chemistry, Nankai University, Tianjin 300071, China; 2. National Pesticide Engineering Research Center （Tianjin）, Tianjin 300071, Chi)

机构地区：[1]南开大学化学学院,元素有机化学国家重点实验室,天津300071 [2]农药国家工程研究中心(天津),天津300071

出　　处：《农药学学报》2018年第4期397-407,共11页Chinese Journal of Pesticide Science

基　　金：国家重点研发计划(2017YFD0200900);国家自然科学基金(31571991);中国博士后科学基金面上项目(2017M611156)

摘　　要：新型杀菌剂的创制在农业可持续发展和克服抗药性中具有重要作用。由于杀菌剂作用机制或靶标是新杀菌剂分子设计合成和创制开发的重要基础,因此作用机制或靶标研究的滞后会阻碍新先导化合物的发现或新品种的创制。鉴于此,本文对目前杀菌剂作用靶标的识别及靶向杀菌剂的分子设计进行了概述。首先阐述了基于转录组学、蛋白质组学的研究和药物亲和层析技术在靶标识别中的应用;其次概述了多学科交叉的方法在分子靶标验证中的应用;最后以strobilurin A为先导的Qo位点抑制剂、以肉桂酸为先导的卵菌抑制剂、以萎锈灵为先导的琥珀酸脱氢酶和植物免疫激活剂等不同类型的靶向杀菌剂为例进行了举例说明。The development of novel fungicide is important for overcoming the resistance and ensuring the sustainable development of agricultural production. The knowledge about the mode of action and the target of the fungicides is of great importance for the design of novel fungicide molecular and the development of novel fungcides. The slow development in those field will restrict the discovery of novel fungcide precursor and the development of new fungicide. In this review, the application of target recognition and proteimic studies in target reconition and identification was elucidated. Firstly, the application of transcriptomic, proteomics-based research and drug affinity chromatography was summaried. Secondly, the application of multidisciplinary approaches in molecular target validation was reviewed. In addtion, the development and molecular design of fungicides of different types with different targets were also introduced in details, using the precursor of Qo inhibitor-strobilurin A, the precursor of oomycetes inhibitor-the cinnamic acid, and the precursor of succinic dehydrogenase inhibitor-the verticillium as examples.

关 键 词：靶向杀菌剂 作用机制 杀菌剂靶标识别 农药分子设计 新农药创制 

分 类 号：S481.1[农业科学—农药学]