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首页> 外文期刊>Biophysical Chemistry: An International Journal Devoted to the Physical Chemistry of Biological Phenomena >Insights into the synergistic mechanism of target resistance: A case study of N. lugens RDL-GABA receptors and fipronil
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Insights into the synergistic mechanism of target resistance: A case study of N. lugens RDL-GABA receptors and fipronil

机译：识别靶耐药协同机制：对N.Lugens RDL-GABA受体和FIPRONIL的案例研究

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摘要

It is known that a single mutation exerts moderate resistance to pesticide, while double mutations (DM) cause severe resistance problem through synergistic effect, and even result in failure application of pesticides. However, little is known about how double mutations would synergistically cause much high resistance level. In this work, computational studies were performed on the interaction of fipronil with N. lugens RDL-GABA receptors, to see how single and double mutations changed receptor structure properties and then conferred distinct resistance levels. The A2'S mutation displayed relative weak influence on receptor structure properties. The R0'Q mutation, which has not been detected in the absence of A2'S, however could deeply alter the electrostatic potential around the inner pore region and significantly narrow the bottom region around -2'Pro. For the DM system, the synergistic effect of two mutations lead to similar pore diameters to the WT system, except for the slightly reduced middle part. Docking study and binding free energy calculation revealed that fipronil displayed binding potencies in the order of WT > A2'S > R0'Q > DM systems, coinciding well with the reported fipronil sensitivity trends and resistance levels.
机译：已知单一突变对农药施加中度抗性，而双重突变（DM）通过协同效应引起严重的抗性问题，甚至导致杀虫剂的失效应用。然而，关于双重突变如何协同造成高抗性水平的知识几乎熟知。在这项工作中，对FIPRONIL与N.Lugens RDL-GABA受体的相互作用进行计算研究，以了解单一和双突变如何改变受体结构性能，然后赋予明显的抗性水平。 A2的突变显示对受体结构性质的相对弱影响。然而，在没有A2的情况下未检测到的R0'Q突变可以深入地改变内孔区域周围的静电电位，并且在-2'PRO周围显着缩小底部区域。对于DM系统，两个突变的协同效应导致与WT系统相似的孔径，除了略微减少的中间部分。对接研究和结合自由能量计算显示，FIPRONIL按WT> A2> R0'Q> DM系统的顺序显示绑定型效力，与报道的近荣敏感度趋势和阻力水平相吻合。

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