昆虫GPCR是否是理想的下一代农药：机遇与挑战,The FEBS Journal

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昆虫GPCR是否是理想的下一代农药：机遇与挑战
The FEBS Journal ( IF 5.5 ) Pub Date : 2021-01-08 , DOI: 10.1111/febs.15708
Necla Birgül Iyison ₁ , Aida Shahraki ₁ , Kübra Kahveci ₁ , Mustafa Barbaros Düzgün ₁ , Gökhan Gün ₁

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人口的增长，加上现有农药的低效率和低副作用，加剧了对开发下一代农药的迫切需求。在可用的方法中，针对无脊椎动物G蛋白偶联受体（GPCR）的策略非常有前途，因为这些受体是内源性神经肽/神经调节剂的靶标，与受体结合后会引起昆虫生理学的深刻变化。因此，探索GPCR调节剂在开发靶向下一代农药方面具有巨大潜力。尽管此类替代农药潜力巨大，但迄今为止，只有一种批准的化合物Amitraz可通过GPCR章鱼胺受体传达其抗虫活性。在这里，我们回顾一下农药发展的现状，与常规农药化合物相关的危害，涉及下一代农药的替代策略，GPCR的结构特征，以及针对无脊椎动物这一超家族成员开发抗虫剂的机遇与挑战。总之，我们强调，如果没有更多的基因组和转录组数据来增进我们对肽信号传导途径复杂网络的了解，就无法充分利用GPCR的潜力。我们认为获得重要生理目标GPCR的三维（3D）结构数据至关重要，并鼓励读者使用最新技术针对无脊椎动物这一超家族成员开发抗虫剂的机遇与挑战。总之，我们强调，如果没有更多的基因组和转录组数据来增进我们对肽信号传导途径复杂网络的了解，就无法充分利用GPCR的潜力。我们认为获得重要生理目标GPCR的三维（3D）结构数据至关重要，并鼓励读者使用最新技术针对无脊椎动物这一超家族成员开发抗虫剂的机遇与挑战。总之，我们强调，如果没有更多的基因组和转录组数据来增进我们对肽信号传导途径复杂网络的了解，就无法充分利用GPCR的潜力。我们认为获得重要生理目标GPCR的三维（3D）结构数据至关重要，并鼓励读者使用最新技术通过计算机方法，例如虚拟筛选来发现新的农药化合物。

"点击查看英文标题和摘要"

Are insect GPCRs ideal next‐generation pesticides: opportunities and challenges

The increasing human population, combined with low inefficiency and adverse effects of available pesticides, has magnified the urgent need of developing next‐generation pesticides. Among the available approaches, strategies targeting invertebrate G protein‐coupled receptors (GPCRs) are very promising as these receptors are the targets of endogenous neuropeptides/neuromodulators that upon binding to their receptors induce profound changes in insect physiology. Therefore, exploring GPCR regulators has great potential in the development of targeted next‐generation pesticides. Despite the great potential of such alternative pesticides, so far there has been only one approved compound, Amitraz, which conveys its anti‐pest activity via the GPCR Octopamine receptor. Here, we review the current status of pesticide development, hazards associated with conventional pesticide compounds, alternative strategies that involve next‐generation of pesticides, structural features of GPCRs, and opportunities and challenges of targeting the members of this superfamily in invertebrates to develop anti‐pest agents. In conclusion, we emphasize that the potential of GPCRs cannot be utilized in full without more genomic and transcriptomic data to improve our understanding of the complex network of peptidergic signaling pathways. We argue how vital it is to obtain three‐dimensional (3D) structural data on physiologically important target GPCRs and encourage the readers to use the state of the art in silico methods such as virtual screening for the discovery of new pesticide compounds.

更新日期：2021-01-08

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