数字农科院2.0

The amino acid Ser223 acts as a key site for the binding of Thrips palmi α1 nicotinic acetylcholine receptor to neonicotinoid insecticides

文献类型: 外文期刊

作者: Kun Zhang;Jianwen Chen;Huixiu Huang;Huiqi Wen;Jingfang Yang;Junjie Geng;Shaoying Wu

作者机构:

关键词: Computer simulation;Heterologous expression;Neonicotinoids;Nicotinic acetylcholine receptors;Thrips palmi

期刊名称: Pesticide Biochemistry and Physiology

ISSN: 0048-3575

年卷期: 2025 年 213 卷

页码:

收录情况: SCIE(2025版)

摘要: Thrips palmi (Karny) is a devastating pest on melons and vegetables worldwide. Neonicotinoids, which act on nicotinic acetylcholine receptors (nAChRs), are among the most effective insecticides for thrips control. For the high neonicotinoids resistance in T. palmi, it is urgent to clarify the main target subunits of neonicotinoid action and the molecular mechanism of subunits binding insecticides. In this study, we cloned two α subunits (α1 and α2) of T. palmi. T. palmi α1/ Rattus norregicus β2 and T. palmi α2/ R. norregicus β2 nAChR subtypes were successfully heterologous expressed in Xenopus laevis oocytes, respectively. After stimulation of the two receptor subtypes by each of the three neonicotinoids (imidacloprid, clothianidin and dinotefuran), for Tpα1/rβ2, dinotefuran showed the highest agonist affinity (pEC50) and efficacy (Imax), whereas for Tpα2/rβ2, dinotefuran showed the lowest agonist affinity, and the highest agonist efficacy was clothianidin. Overall, the agonist affinity and efficacy of Tpα1/rβ2 were greater than that of Tpα2/rβ2, which proved that α1 subunit of T. palmi is the main target of neonicotinoids. Computer simulation and electrophysiological experiment results showed the different responses of the same neonicotinoid to two nAChR subtypes were mainly due to the difference between Lys220/Ser223 in Tpα1 and Arg223/Pro226 in Tpα2, with Ser223 identified as the key binding site. This study revealed that the nAChR subunit of T. palmi binds to the key amino acid residues of neonicotinoid insecticides, which provides the basis for the subsequent design and synthesis of green and efficient specific insecticides.

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