Ion channels as insecticide targets.
Ion channels as insecticide targets.
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DOI：
10.1080/01677063.2016.1229781
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发表时间：
2016-09
影响因子：
1.9
通讯作者：
Bass C
中科院分区：
文献类型：
--
作者：
Ffrench-Constant RH;Williamson MS;Davies TG;Bass C
离子通道仍然是大多数小分子杀虫剂的主要靶标。本文综述了异源表达受体的亚基组成如何决定其杀虫剂特异性药理作用，以及表达受体的药理作用与昆虫神经系统中的药理作用有何不同。我们发现，一些受体的杀虫剂特异性药理，比如含有RDL编码的GABA受体亚基的受体，可以用很少的自然产生的亚基来表达。相比之下，工作人员甚至难以表达具有功能的昆虫烟碱型乙酰胆碱受体(NAChRs)，因此工作往往依赖于脊椎动物受体亚单位的表达。我们还检查了与杀虫剂耐药性相关的突变，例如在对映体编码的电压门控钠通道中的突变，可以揭示杀虫剂结合位点和作用模式的细节。特别是，我们检查是否在杀虫剂结合部位和/或在变构影响受体的药物偏好构象的部位存在突变。我们还讨论了兰尼定受体作为新近开发的联胺的靶点。最后，我们检查了编码这些受体亚单位的基因的致命性，并讨论了这可能如何决定所发现的抗药性相关突变的保守程度。
Ion channels remain the primary target of most of the small molecule insecticides. This review examines how the subunit composition of heterologously expressed receptors determines their insecticide-specific pharmacology and how the pharmacology of expressed receptors differs from those found in the insect nervous system. We find that the insecticide-specific pharmacology of some receptors, like that containing subunits of the Rdl encoded GABA receptor, can be reconstituted with very few of the naturally occurring subunits expressed. In contrast, workers have struggled even to express functional insect nicotinic acetylcholine receptors (nAChRs), and work has therefore often relied upon the expression of vertebrate receptor subunits in their place. We also examine the extent to which insecticide-resistance-associated mutations, such as those in the para encoded voltage-gated sodium channel, can reveal details of insecticide-binding sites and mode of action. In particular, we examine whether mutations are present in the insecticide-binding site and/or at sites that allosterically affect the drug preferred conformation of the receptor. We also discuss the ryanodine receptor as a target for the recently developed diamides. Finally, we examine the lethality of the genes encoding these receptor subunits and discuss how this might determine the degree of conservation of the resistance-associated mutations found.
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