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Ion channels and G protein-coupled receptors as targets for invertebrate pest control: from past challenges to practical insecticides.
Bioscience, Biotechnology, and Biochemistry ( IF 1.6 ) Pub Date : 2021-06-24 , DOI: 10.1093/bbb/zbab089
Yoshihisa Ozoe 1, 2
Affiliation  

In the late 1970s, we discovered that toxic bicyclic phosphates inhibit the generation of miniature inhibitory junction potentials, implying their antagonism of γ-aminobutyric acid (GABA) receptors (GABARs; GABA-gated chloride channels). This unique mode of action provided a strong incentive for our research on GABARs in later years. Furthermore, minor structural changes conferred insect GABAR selectivity to this class of compounds, convincing us of the possibility of GABARs as targets for insecticides. Forty years later, third-generation insecticides acting as allosteric modulator antagonists at a distinctive site of action in insect GABARs were developed. G protein-coupled receptors (GPCRs) are also promising targets for pest control. We characterized phenolamine receptors functionally and pharmacologically. Of the tested receptors, β-adrenergic-like octopamine receptors were revealed to be the most sensitive to the acaricide/insecticide amitraz. Given the presence of multiple sites of action, ion channels and GPCRs remain potential targets for invertebrate pest control.

中文翻译:

离子通道和 G 蛋白偶联受体作为无脊椎动物害虫控制的目标:从过去的挑战到实用的杀虫剂。

在 1970 年代后期,我们发现有毒的双环磷酸盐会抑制微型抑制性连接电位的产生,这意味着它们会拮抗 γ-氨基丁酸 (GABA) 受体(GABAR;GABA 门控氯离子通道)。这种独特的作用方式为我们后来对 GABAR 的研究提供了强大的动力。此外,微小的结构变化赋予此类化合物昆虫 GABAR 选择性,使我们相信 GABAR 作为杀虫剂靶标的可能性。四十年后,第三代杀虫剂在昆虫 GABAR 的独特作用位点作为变构调节剂拮抗剂被开发出来。G 蛋白偶联受体 (GPCR) 也是有害生物控制的有希望的目标。我们在功能和药理学上表征了酚胺受体。在测试的受体中,β-肾上腺素能样章鱼胺受体被证明对杀螨剂/杀虫剂双甲脒最敏感。鉴于存在多个作用位点,离子通道和 GPCR 仍然是无脊椎动物害虫控制的潜在目标。
更新日期:2021-06-24
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