Taylor Robert W, Romaine Ian M, Liu Chao, Murthi Poornima, Jones Patrick L, Waterson Alex G, Sulikowski Gary A, Zwiebel Laurence J
Department of Biological Sciences, Vanderbilt Institute of Chemical Biology, Vanderbilt University, Nashville, Tennessee 37235, United States.
ACS Chem Biol. 2012 Oct 19;7(10):1647-52. doi: 10.1021/cb300331z. Epub 2012 Aug 27.
Agonism of insect odorant receptor (OR) cation channels may represent a new strategy for the manipulation of destructive insect olfactory-driven behaviors. We have explored the chemical space around VUAA1, the first in class agonist of the obligate OR co-receptor ion channel (Orco), and describe novel compound analogues with increased potency across insect taxa. Functional analyses reveal several of these VUAA1 structural analogues display significantly greater potency as compared to the activity of the previously described active compounds in mobility-based behavioral assays on mosquito larvae.
激活昆虫气味受体（OR）阳离子通道可能代表了一种控制具有破坏性的昆虫嗅觉驱动行为的新策略。我们探索了VUAA1周围的化学空间，VUAA1是专性OR共受体离子通道（Orco）的首个同类激动剂，并描述了在昆虫类群中效力增强的新型化合物类似物。功能分析表明，与之前描述的活性化合物在基于移动性的蚊虫幼虫行为试验中的活性相比，这些VUAA1结构类似物中有几种显示出显著更高的效力。
