Despite years of use as commercial herbicides, it is still unclear how dinitroanilines interact with tubulin, how they cause microtubule disassembly, and why they are selectively active against plant and protozoan tubulin. In this work, through a series of computational studies, a common binding site of oryzalin, trifluralin, and GB-II-5 on apicomplexan and kinetoplastid alpha-tubulin is proposed. Furthermore, to investigate how dinitroanilines affect tubulin dynamics, molecular dynamics simulations of Leishmania alpha-tubulin with and without a bound dinitroaniline are performed. The results obtained provide insight into the molecular mechanism by which these compounds interact with tubulin and function to prevent microtubule assembly. Finally, to aid in the design of effective parasitic microtubule inhibitors, several novel dinitroaniline analogues are evaluated. The location of the binding site and the relative binding affinities of the dinitroanilines all agree well with experimental data.

译文

尽管多年用作商业除草剂,但仍不清楚二硝基苯胺如何与微管蛋白相互作用,它们如何引起微管分解以及为什么它们对植物和原生动物微管蛋白具有选择性活性。在这项工作中,通过一系列的计算研究,提出了米黄素,三氟拉林和GB-II-5在apicomplexan和运动质体α-微管蛋白上的共同结合位点。此外,为了研究二硝基苯胺如何影响微管蛋白动力学,进行了结合和不结合二硝基苯胺的利什曼原虫α-微管蛋白的分子动力学模拟。获得的结果提供了对这些化合物与微管蛋白相互作用并防止微管装配的分子机制的深入了解。最后,为帮助设计有效的寄生微管抑制剂,对几种新型的二硝基苯胺类似物进行了评估。二硝基苯胺的结合位点的位置和相对结合亲和力都与实验数据很好地吻合。

+1
+2
100研值 100研值 ¥99课程
检索文献一次
下载文献一次

去下载>

成功解锁2个技能,为你点赞

《SCI写作十大必备语法》
解决你的SCI语法难题!

技能熟练度+1

视频课《玩转文献检索》
让你成为检索达人!

恭喜完成新手挑战

手机微信扫一扫,添加好友领取

免费领《Endnote文献管理工具+教程》

微信扫码, 免费领取

手机登录

获取验证码
登录