标识虫的普罗克托林受体和设计的普罗克托林类似物
Tai-Tian Xiong1,2, Yi-Ning Lu1,2, Jiabin Pan1
1Key Laboratory of Animal Biodiversity Conservation and Integrated Pest Management, Institute of Zoology, Chinese Academy of Sciences, Beijing, China.
Pest management science
|August 8, 2025
概括
研究人员确定了虫前列素受体 (LmProcR),并预测了它的结构. 修改后的普罗克托林类似物,特别是与N-终端d-alanine,显示增强的myotropic活动,为新的杀虫剂铺平了道路.
科学领域:
- 昆虫生理学 昆虫生理学
- 分子生物学分子生物学
- 结构生物学是结构生物学.
背景情况:
- 普罗克托林 (Proctolin) 是昆虫和甲类动物中的一种神经,具有显著的肌性活性.
- 普罗克托林受体首次被确定在虫中,与其他昆虫中发现的假定受体相结合,但缺乏功能验证.
研究的目的:
- 实验性地识别和描述虫Locusta migratoria (LmProcR) 中的普罗克托林受体.
- 阐明前列素结合和信号传递的结构基础.
- 设计和测试具有增强活性的新型普罗克托林类似物.
主要方法:
- 在Locusta migratoria.中对LmProcR的实验性鉴定.
- 测量细胞内离子 (Ca2+) 度和beta-arrestin-2转位在前科林刺激后.
- 基于AlphaFold3的LmProcR-proctolin复合物的结构预测.
- 设计和合成N-终端修饰的普罗克托林类似物.
- 对类似物质对虫前收缩的肌性活性评估.
主要成果:
- 确定了lmProcR,并证明它通过Ca2+增加和β-arrestin-2转位调解了普罗克托林的作用.
- 预测的结构揭示了lmProcR作为一个G蛋白合受体,在一个跨膜口袋中与proctolin结合.
- 普罗克托林的Arg1下方的腔体表明可能存在N-终端修饰.
- N-终端修饰的普罗克托林类型,特别是与d-alanine,表现出显著增强的肌性活性.
结论:
- 这项研究提供了第一次实验性识别和对虫前列素受体 (LmProcR) 的结构洞察.
- 结构信息有助于设计新型的前列素仿真剂.
- 这些发现为开发新的基于普罗克托林的杀虫剂奠定了基础.
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