• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>RSC Advances >Synthesis and biological activity study of the retro-isomer of RhTx against TRPV1
【24h】

Synthesis and biological activity study of the retro-isomer of RhTx against TRPV1

机译：TRPV1 rHTX r rtro-isomer的合成与生物活性研究

获取原文
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

TRPV1 is a ligand-gated ion channel and plays an important role in detecting noxious heat and pain with an unknown mechanism. RhTx from Chinese red-headed centipede activates the TRPV1 channel through the heat activation pathway by binding to the outer pore region, and causes extreme pain. Here, we synthesized RhTx and its retro-isomer RL-RhTx. Their structures were investigated by their circular dichroic spectra and NMR spectra. The effect of RhTx and RL-RhTx on the currents of wild-type and mutants of TRPV1 indicated that RL-RhTx have comparable TRPV1 activation responses to RhTx. A mutagenesis study showed that four TRPV1 residues, including Leu461, Asp602, Tyr632 and Thr634, significantly contributed to the activation effects of RL-RhTx and RhTx, and both peptides probably bind with TRPV1 in similar binding modes. As a novel TRPV1 activator, RL-RhTx provides an essential powerful tool for the investigation of activation mechanisms of TRPV1.
机译：TRPV1是一种配体门控离子通道，在检测有害的机制检测有氧的热量和疼痛方面起着重要作用。来自中国红蜈蚣的rhTX通过与外孔区域结合来激活TRPV1通道通过热激活途径，并引起极端疼痛。在此，我们合成rhtx及其复古异构体R1-rhtx。通过其圆形二向色谱和NMR光谱研究了它们的结构。 rhTX和R1-rhTX对TRPV1野生型和突变体电流的影响表明RL-rhTX具有与RHTX的相当的TRPV1激活响应。诱变研究表明，四个TRPV1残基，包括Leu461，ASP602，Tyr632和Tr634，显着导致RL-rhTx和rhTx的活化效果，并且两种肽可能以类似的结合模式与TRPV1结合。作为新型TRPV1激活剂，RL-RHTX为研究TRPV1的激活机制提供了一个基本的强大工具。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号