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The Pheromone Biosynthesis Activating Neuropeptide (PBAN) Receptor of Heliothis virescens: Identification Functional Expression and Structure-Activity Relationships of Ligand Analogs

机译:拟南芥的信息素生物合成激活神经肽(PBAN)受体:配体类似物的鉴定功能表达和结构-活性关系。

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摘要

Pheromone biosynthesis activating neuropeptide (PBAN) promotes synthesis and release of sex pheromones in moths. We have identified and functionally expressed a PBAN receptor from Heliothis virescens (HevPBANR) and elucidated structure-activity relationships of PBAN analogs. Screening of a larval CNS cDNA library revealed three putative receptor subtypes and nucleotide sequence comparisons suggest they are produced through alternative splicing at the 3’-end. RT-PCR amplified preferentially HevPBANR-C from female pheromone glands. CHO cells expressing HevPBANR-C are highly sensitive to PBAN and related analogs, especially those sharing the C-terminal pentapeptide core, FXPRLamide (X = T, S or V). Alanine replacements in the C-terminal hexapeptide (YFTPRLamide) revealed the relative importance of each residue in the active core as follows, R5>L6>F2≫P4>T3≫Y1. This study provides a framework for the rational design of PBANR-specific agonists and/or antagonists that could be exploited for disruption of reproductive function in agriculturally important insect pests.
机译:信息素生物合成激活神经肽(PBAN)促进飞蛾中性信息素的合成和释放。我们已经鉴定并功能表达了来自Heliothis virescens(HevPBANR)的PBAN受体,并阐明了PBAN类似物的构效关系。幼虫CNS cDNA文库的筛选显示了三种假定的受体亚型,核苷酸序列比较表明它们是通过3'端的选择性剪接产生的。 RT-PCR优先从雌性信息素腺中扩增HevPBANR-C。表达HevPBANR-C的CHO细胞对PBAN和相关类似物高度敏感,尤其是那些共享C末端五肽核心FXPRLamide(X = T,S或V)的细胞。 C端六肽(YFTPRLamide)中的丙氨酸置换揭示了活性核心中每个残基的相对重要性,如下所述,R 5 6 2 ≫P 4 3 ≫Y 1 。这项研究为合理设计PBANR特异性激动剂和/或拮抗剂提供了一个框架,可用于破坏农业重要害虫的生殖功能。

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