杀虫剂分子靶标烟碱型乙酰胆碱受体研究进展

昆虫烟碱型乙酰胆碱受体(nicotinic acetylcholine receptors,nAChRs)广泛分布于昆虫中枢神经系统,是杀虫剂作用的主要靶标。目前昆虫中该受体的天然亚基组成尚不完全明确。果蝇的任意α亚基与脊椎动物的一个β亚基共表达是目前最好的异源表达模型,但仍然急需新的研究工具,研究表明一些与受体相关的蛋白质影响着表达。胞内磷酸化的调节作用为今后受体药理学特性的研究提供了新方向。受体亚基上一些关键氨基酸在新烟碱杀虫剂对受体的选择作用中起重要作用。在对吡虫啉抗性的褐飞虱种群中找到了与抗性相关的突变位点,这为新烟碱类杀虫剂靶标不敏感性研究提供了直接证据。对昆虫烟碱型乙酰胆碱受体的分子多样性、功能表达、胞内调节机制、受体与杀虫剂的选择作用及其抗性分子机理等的研究进展进行了综述。

Advances in the Molecular Target for Insecticides ofNicotinic Acetylcholine Receptors

Insect nicotinic acetylcholine receptors(nAChRs)are molecular targets of insecticides, they widely expressed in the central nervous system.The natural subunit composition of nAChRs is not yet entirely clear.Coexpression of any Drosophila a subunit with a vertebrate β subunit constitutes the best available heterologous expression model at present,but still need to provide new robust heterologous expression research tool.Some important nACh receptor-associated proteins effect the robust expression in cell lines.Insect nACh receptor can be modulated by intracellular phosphorylation mechanisms,which offers a new approach to studying insect nACh receptor pharmacology.Amino acids within the subunits have a role in the selectivity of neonicotinoids for insect nACh receptor.Researching on brown planthopper found a mutation conferring target-site resistance to imidacloprid,this study provides direct evidence for target insensitivity to neonicotinoid insecticide.The latest progress on the molecular diversity,functional expression,intracellular regulation mechanisms,selectivity of insecticides for insect nAChRs and target resistance mechanisms were reviewed.