Center for Medical, Agricultural, and Veterinary Entomology, USDA-ARS, Gainesville, FL 32608, USA.
Foresight Science and Technology, Hopkinton, MA 01748, USA.
Int J Mol Sci. 2023 Sep 12;24(18):13978. doi: 10.3390/ijms241813978.
Receptor-interference (Receptor-i) is a novel technology used to identify bioactive peptides as agonists or antagonists against a specific receptor, primarily targeting G-protein-coupled receptors (GPCRs). Using Receptor-i methodology, we targeted the pheromone biosynthesis activating neuropeptide receptor (PBAN-R) of the red imported fire ant (). Based on previous studies, we selected four bioactive peptides cyclized with two cysteines: CVKLGSHFC, CIQQGSHFC, CERVGSHFC, and CMARYMSAC, and we conducted small-scale feeding bioassays, measuring fire ant worker mortality. All peptides reduced ant survival; however, CMARYMSAC (MARY) and CIQQGSHFC (IQQG) were the most effective and were selected for feeding trials against large, fully functional fire ant field colonies containing queen, brood, and up to 8000 workers. At the end of the experiment, day 84, synthetic peptide MARY killed over 80% of the workers and two of four queens. IQQG killed over 70% of the workers and three of four queens. The surviving two MARY queens lost an average of 21% of their starting weight. The surviving IQQG queen lost 31% of its weight. In contrast, control colony queens gained an average of 11% of their starting weight. These results provide proof-of-concept for the Receptor-i technology and will synergize applications to other agricultural and medical pests.
受体干扰（Receptor-i）是一种用于鉴定生物活性肽作为针对特定受体的激动剂或拮抗剂的新技术，主要针对 G 蛋白偶联受体（GPCR）。使用 Receptor-i 方法，我们针对红火蚁（）的信息素生物合成激活神经肽受体（PBAN-R）。基于先前的研究，我们选择了四个带有两个半胱氨酸环化的生物活性肽：CVKLGSHFC、CIQQGSHFC、CERVGSHFC 和 CMARYMSAC，并进行了小规模的喂养生物测定，测量了红火蚁工蚁的死亡率。所有肽都降低了蚂蚁的存活率；然而，CMARYMSAC（MARY）和 CIQQGSHFC（IQQG）是最有效的，被选择用于针对包含蚁后、幼虫和多达 8000 名工蚁的大型、功能齐全的红火蚁野外群体的喂养试验。在实验结束时，第 84 天，合成肽 MARY 杀死了超过 80%的工蚁和 4 只蚁后中的 2 只。IQQG 杀死了超过 70%的工蚁和 4 只蚁后中的 3 只。幸存的 2 只 MARY 蚁后体重平均损失了 21%。幸存的 IQQG 蚁后体重减轻了 31%。相比之下，对照群体的蚁后体重平均增加了 11%。这些结果为 Receptor-i 技术提供了概念验证，并将与其他农业和医学害虫的应用协同增效。
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