昆虫鱼尼丁受体结构功能及抗性机制研究进展

    Advances in structural and functional studies of the insect ryanodine receptor and the related resistance mechanisms

    • 摘要: 双酰胺类杀虫剂可用于控制包括鳞翅目、鞘翅目等在内的多种重要农业害虫,作用机制新颖且对非靶标生物安全低毒,已成为目前全世界销量最高的杀虫剂品种之一。近期在抗性昆虫种群里发现的突变大幅降低了其效能,对各国的农业生产造成了巨大的经济损失。双酰胺类杀虫剂的分子靶标鱼尼丁受体作为近年来最受关注的新型热点靶标被广泛研究。本文总结了昆虫鱼尼丁受体结构和功能研究方面的最新发现,包括1) 双酰胺类杀虫剂在昆虫鱼尼丁受体上的结合位点和作用方式;2) 抗性突变对靶标结构功能的影响;3) 双酰胺类杀虫剂结合位点以外的潜在新作用位点;4) 传统和新作用位点在靶标和非靶标生物鱼尼丁受体上的结构差异,并对基于鱼尼丁受体结构的新一代绿色杀虫剂设计开发进行了展望。

       

      Abstract: Diamide insecticides are used to control a variety of destructive agricultural Lepidopteran and Coleopteran pests. They possess a novel mechanism of action and are safe for nontarget organisms; thus, they have become among the best-selling insecticides in the world. Mutations recently discovered in resistant insect populations significantly reduce their efficacy, causing enormous economic losses to agricultural production in various countries. The molecular target of diamide insecticides, the ryanodine receptor (RyR), has been widely studied as a new hot target and has received much attention in recent years. The latest findings on the structure and function of insect RyRs, including 1) the binding site and mode of action of diamide insecticides, 2) the impacts of resistance mutations on the structure and function of RyRs, 3) potential new target sites on RyRs other than the diamide insecticides binding site, and 4) structural differences of the classic and new target sites between the target and nontarget organisms, were summarized in the review. Finally, how the progress in RyR structural biology might facilitate the design and development of a new generation of green pesticides was also discussed.

       

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