Functional agonism of insect odorant receptor ion channels

Functional agonism of insect odorant receptor ion channels
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DOI:
10.1073/pnas.1102425108
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发表时间:
2011-05-24
影响因子:
11.1
通讯作者:
Zwiebel, Laurence J.
Zwiebel, Laurence J.
中科院分区:
综合性期刊1区
文献类型:
--
作者:
Jones, Patrick L.;Pask, Gregory M.;Zwiebel, Laurence J.

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在昆虫中,气味线索是通过不同的气味受体(OR)家族来区分的。功能性OR复合物由传统的气味剂结合OR和在昆虫分类群中高度保守的非传统辅助受体(Orco)组成。最近的报道将昆虫的OR表征为离子通道,但信号传导的确切机制仍不清楚。我们报告的Orco家族激动剂,VUAA1,使用冈比亚按蚊辅助受体(AgOrco)和其他直系同源物的识别和表征。这些研究表明,Orco家族可以在没有气味结合OR的情况下形成功能性离子通道,此外,还为进一步研究昆虫OR信号提供了一流的激动剂。鉴于Orco家族的非凡保护和广泛表达,VUAA1代表了一个强大的新化合物家族,可用于破坏有害昆虫,农业害虫和疾病媒介的破坏性行为。
In insects, odor cues are discriminated through a divergent family of odorant receptors (ORs). A functional OR complex consists of both a conventional odorant-binding OR and a nonconventional coreceptor (Orco) that is highly conserved across insect taxa. Recent reports have characterized insect ORs as ion channels, but the precise mechanism of signaling remains unclear. We report the identification and characterization of an Orco family agonist, VUAA1, using the Anopheles gambiae coreceptor (AgOrco) and other orthologues. These studies reveal that the Orco family can form functional ion channels in the absence of an odor-binding OR, and in addition, demonstrate a first-in-class agonist to further research in insect OR signaling. In light of the extraordinary conservation and widespread expression of the Orco family, VUAA1 represents a powerful new family of compounds that can be used to disrupt the destructive behaviors of nuisance insects, agricultural pests, and disease vectors alike.