分子模型
分子动力学
分子描述符
有害生物分析
对接(动物)
农业害虫
计算生物学
化学
生物化学
生物
活动站点
分子标记
结构-活动关系
病虫害综合治理
组合化学
同源建模
药物发现
结合位点
合理设计
生物技术
立体化学
作者
Fernanda F. de Souza,Juliana F. Vilachã,Othon S. Campos,Heberth de Paula
标识
DOI:10.3390/targets4010001
摘要
Acetylcholinesterase (AChE) is an important molecular target in the development of insecticides, but due to also being found in the human body, it is necessary to characterize the inhibitory profile of compounds to achieve selectivity. In this study, we employed molecular modeling and 3D-QSAR approaches to identify novel compounds that inhibit AChE1 in Bemisia tabaci, a common agricultural pest in tropical and subtropical crops. We conducted molecular docking simulations and quantitative structure–activity relationship analysis (QSAR) to identify compounds with potential inhibitory activity and to develop a predictive model for the activity of these new compounds. The validated model demonstrated remarkable predictive performance. Using the model, we screened a library of novel moieties in favorable regions of the most active molecules in the dataset and identified promising candidates, including FS168. We performed molecular dynamics simulations with FS168 bound to the AChE1 of B. tabaci and observed stabilization and interaction with important catalytic amino acids, indicating a potential inhibition mechanism. Our results showcase the potential of combining molecular modeling and 3D-QSAR approaches for discovering new potential AChE1 inhibitors in Bemisia tabaci as selective agrochemicals.
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