首页> 外国专利> DNA MOLECULES ENCODING CTENOCEPHALIDES FELIS GLUTAMATE GATED CHLORIDE CHANNELS

DNA MOLECULES ENCODING CTENOCEPHALIDES FELIS GLUTAMATE GATED CHLORIDE CHANNELS

机译:DNA分子编码胆汁谷胱甘肽门控氯化物通道

摘要

To date, L-glutamate-gated chloride (GluC1) channels have been observed only in invertebrate organisms. Modulators of this channel (either agonists or antagonists) will interfere with neurotransmission. For example, agents such as avermectins activate the GluCl, causing paralysis due to blocking of neurotransmitter release, resulting in death of the organism. Because GluCl channels are invertebrate specific, they are excellent targets for the discovery of novel insecticides, anthelminths and parasiticides that will display a marked safety profile because of the lack of mechanism based toxicity in vertebrate organisms. The present specification discloses isolation of a cDNA clone from the cat flea Ctenocephalides felis (CfGluCl-1) that encodes a L-glutamate-gated chloride channel. Heterologous expression of CfGluCl-1 cRNA in Xenopus oocytes results in robust expression of a L-glutamate-gated chloride current and the channel is activated and potentiated by avermectins. The expression of CfGluCl-1 in a heterologous expression system is useful to screens for novel GluCl channel agonists and antagonists. Additionally, this specification discloses improved methods of screening for GluCl channel modulators.
机译:迄今为止,仅在无脊椎动物中观察到L-谷氨酸门控氯化物(GluC1)通道。该通道的调节剂(激动剂或拮抗剂)将干扰神经传递。例如,诸如阿维菌素之类的试剂激活GluCl,由于阻止神经递质释放而引起麻痹,从而导致生物体死亡。因为GluCl通道是无脊椎动物特异性的,所以它们是发现新型杀虫剂,驱虫药和杀寄生虫剂的极好靶标,由于脊椎动物中缺乏基于机理的毒性,它们将显示出明显的安全性。本说明书公开了从猫跳蚤Ctenocephalides felis(CfGluCl-1)中分离编码L-谷氨酸门控氯化物通道的cDNA克隆。 CfGluCl-1 cRNA在非洲爪蟾卵母细胞中的异源表达导致L-谷氨酸门控氯化物电流的稳健表达,并且通道被阿维菌素激活并增强。 CfGluCl-1在异源表达系统中的表达可用于筛选新型GluCl通道激动剂和拮抗剂。另外,本说明书公开了筛选GluCl通道调节剂的改进方法。

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