Division of Genomics Resources, ICAR-National Bureau of Agricultural Insect Resources, Bengaluru 560024, Karnataka, India.
Division of Genomics Resources, ICAR-National Bureau of Agricultural Insect Resources, Bengaluru 560024, Karnataka, India.
Comput Biol Chem. 2018 Dec;77:240-250. doi: 10.1016/j.compbiolchem.2018.09.004. Epub 2018 Sep 8.
Acetylcholinesterase-1 (AChE1) is a vital enzyme involved in neurotransmission and represents an attractive insecticide-target for organophosphates and carbamates in Plutella xylostella (Linneaus), an important pest of cruciferous crops worldwide. However, insecticide-resistance often occurs due to mutations, making many organophosphates and carbamates ineffective. In particular, A298S and G324A mutations in AChE1 significantly lower the binding affinity of insecticides. In the present study, the wild-type and mutant AChE1 structures were constructed and their structural stabilities, residual flexibilities were investigated through molecular dynamics simulations. Subsequently, the structural and energetic changes responsible for the insecticide-resistance in AChE1 were analyzed using molecular docking. The results of molecular dynamics simulation showed that the mutant AChE1 shows little structural deviation than the wild-type, indicate the structural instability. Furthermore, the docking results demonstrated that these mutations break the intermolecular hydrogen bonding interactions and thereby affect the prothiofos as well as all insecticide binding. Hence, the results could provide some insights into the resistance mechanism of AChE1 in insecticides binding and helpful in the development of novel insecticides that are less susceptible to insecticide-resistance.
乙酰胆碱酯酶 1(AChE1)是一种参与神经传递的重要酶,是小菜蛾(Plutella xylostella)(十字花科作物的重要害虫)中有机磷和氨基甲酸酯类杀虫剂的理想靶点。然而,由于突变,昆虫常常对杀虫剂产生抗药性,使许多有机磷和氨基甲酸酯类杀虫剂失效。特别是 AChE1 中的 A298S 和 G324A 突变显著降低了杀虫剂的结合亲和力。在本研究中,构建了野生型和突变型 AChE1 的结构,并通过分子动力学模拟研究了它们的结构稳定性和剩余柔韧性。随后,通过分子对接分析了导致 AChE1 抗药性的结构和能量变化。分子动力学模拟的结果表明,与野生型相比,突变型 AChE1 的结构偏差很小,表明结构不稳定。此外,对接结果表明这些突变破坏了分子间氢键相互作用,从而影响了丙硫磷以及所有杀虫剂的结合。因此,这些结果可以为 AChE1 在杀虫剂结合中的抗药性机制提供一些见解,并有助于开发不易产生抗药性的新型杀虫剂。