绿色杀虫剂分子靶标研究的难点与挑战  

Challenges and Future Directions for Greener Insecticide Molecular Targets

作　　者：陈威 陈琦 尉迟之光 杨青 Chen Wei;Chen Qi;Yuchi Zhiguang;Yang Qing(State Key Laboratory for Biology of Plant Diseases and Insect Pests/Institute of Plant Protection,Chinese Academy of Agricultural Sciences,Beijing 100193;School of Pharmaceutical Science and Technology,Tianjin University,Tianjin 300072)

机构地区：[1]中国农业科学院植物保护研究所/植物病虫害生物学国家重点实验室,北京100193 [2]天津大学药物科学与技术学院,天津300072

出　　处：《中国科学基金》2020年第4期502-510,共9页Bulletin of National Natural Science Foundation of China

摘　　要：绿色杀虫剂是保证国家粮食安全的战略性物资。随着全球农业的绿色化和可持续化的发展进程,靶标导向并且对人畜和非靶标生物安全的新农药创制已成为该领域研究的必然趋势和制高点,其核心基础是农药分子靶标的创新。一方面,全球超过80%杀虫剂是基于4个晶体结构明确的分子靶标设计的,这一局面导致极高的害虫抗药性;另一方面,分子生物学功能验证技术揭示出大量害虫生长发育所必需的关键基因,如何利用这些资源开发创新的分子靶标是我们面临的挑战。在靶标研究中,获得原子水平的靶标结构信息以及靶标分子与活性小分子之间的相互作用信息是难点。在此背景下,我国有必要尽快建立针对害虫特有而人畜没有的分子靶标挖掘与利用的技术体系,推进安全高效绿色杀虫剂的原始创新。Green insecticides ensure plant protection and thus food supply for a nation in a view of national strategies.To meet the global demands for greener and more sustainable agriculture,developing targetselective insecticides,namely human-and other non-target organism-safe insecticides,has become an inevitable trend and a hot topic.It is highly dependent on novel and greener molecular targets.On the one hand,more than 80% of insecticides are designed based on crystal structures of only four molecular targets,leading to extremely high resistance of pests.On the other hand,rapid progress in biotechnologies such as genome-sequencing and functional verification offers a number of gene candidates,which are crucial for growth and development of pests,for developing novel molecular targets.However,the challenge we are facing is how to make use of these resources to obtain innovative molecular targets.The difficulty in obtaining the atomic-level structural information of target candidates and the interactions between bioactive molecules and molecular targets is another issue.In the latest decades,it is urgent for China to establish a system for green molecular targets’ mining and exploiting,promoting the leading role of China in green insecticides innovation and the industry relevant.

关 键 词：杀虫剂 分子靶标 昆虫生长调节剂 几丁质 鱼尼丁受体 

分 类 号：TQ453[化学工程—农药化工]