Voltage-gated sodium channels as targets for pyrethroid insecticides.

Voltage-gated sodium channels as targets for pyrethroid insecticides.
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DOI:
10.1007/s00249-016-1195-1
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发表时间:
2017-10
期刊:
European biophysics journal : EBJ
影响因子:
--
通讯作者:
Wallace BA
Wallace BA
中科院分区:
其他
文献类型:
--
作者:
Field LM;Emyr Davies TG;O'Reilly AO;Williamson MS;Wallace BA

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拟除虫菊酯类杀虫剂是一组非常成功的化合物,已广泛用于控制农作物的节肢动物害虫以及动物和人类疾病的媒介。不幸的是,这导致了许多物种对化合物的耐药性。已知拟除虫菊酯的作用模式是通过与电压门控钠通道相互作用。了解与通道的结合如何受到引起抗性的氨基酸取代的影响,有助于阐明化合物的作用模式及其对昆虫与哺乳动物以及昆虫与其他节肢动物之间的选择性的分子基础。通道/拟除虫菊酯相互作用的建模,加上在卵母细胞中表达突变通道和研究功能的能力,已经导致了对通道如何发挥作用以及如何设计具有更大物种选择性的新型杀虫剂的认识。
The pyrethroid insecticides are a very successful group of compounds that have been used extensively for the control of arthropod pests of agricultural crops and vectors of animal and human disease. Unfortunately, this has led to the development of resistance to the compounds in many species. The mode of action of pyrethroids is known to be via interactions with the voltage-gated sodium channel. Understanding how binding to the channel is affected by amino acid substitutions that give rise to resistance has helped to elucidate the mode of action of the compounds and the molecular basis of their selectivity for insects vs mammals and between insects and other arthropods. Modelling of the channel/pyrethroid interactions, coupled with the ability to express mutant channels in oocytes and study function, has led to knowledge of both how the channels function and potentially how to design novel insecticides with greater species selectivity.
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