Overview of the Status and Global Strategy for Neonicotinoids
Overview of the Status and Global Strategy for Neonicotinoids
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DOI：
10.1021/jf101303g
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发表时间：
2011-04-13
影响因子：
6.1
通讯作者：
Elbert, Alfred
中科院分区：
文献类型：
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作者：
Jeschke, Peter;Nauen, Ralf;Elbert, Alfred
近年来，新烟碱类杀虫剂已成为现代作物保护中发展最快的一类杀虫剂，广泛用于防治各种吸食和某些咀嚼害虫。作为有效的激动剂，它们选择性地作用于昆虫的烟碱型乙酰胆碱受体(NAChRs)，这是它们的分子靶点。新烟碱类化合物的发现可以被认为是杀虫剂研究的一个里程碑，极大地促进了对昆虫nAChRs功能特性的了解。在这种背景下，乙酰胆碱结合蛋白的晶体结构为设计nAChRs内相应受体配体结合域的同源模型提供了理论基础，为虚拟筛选化学文库和合理设计作用于这些实际相关通道的新型杀虫剂提供了有用的基础。由于新烟碱类杀虫剂对非靶标生物和环境的风险相对较低，新烟碱类杀虫剂具有较高的靶标特异性，以及它们在使用方法上的多样性，这一重要类别必须在全球范围内保持，以实施综合害虫管理战略和害虫抗性管理计划。生命周期管理的创新概念，加上非专利产品的推出，使新烟碱成为杀虫剂市场最重要的化学类别。
In recent years, neonicotinoid insecticides have been the fastest growing class of insecticides in modern crop protection, with widespread use against a broad spectrum of sucking and certain chewing pests. As potent agonists, they act selectively on insect nicotinic acetylcholine receptors (nAChRs), their molecular target site. The discovery of neonicotinoids can be considered as a milestone in insecticide research and greatly facilitates the understanding of functional properties of the insect nAChRs. In this context, the crystal structure of the acetylcholine-binding proteins provides the theoretical foundation for designing homology models of the corresponding receptor ligand binding domains within the nAChRs, a useful basis for virtual screening of chemical libraries and rational design of novel insecticides acting on these practically relevant channels. Because of the relatively low risk for nontarget organisms and the environment, the high target specificity of neonicotinoid insecticides, and their versatility in application methods, this important class has to be maintained globally for integrated pest management strategies and insect resistance management programs. Innovative concepts for life-cycle management, jointly with the introduction of generic products, have made neonicotinoids the most important chemical class for the insecticide market.