...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Channels >Allosteric regulation of pentameric ligand-gated ion channels An emerging mechanistic perspective
【24h】

Allosteric regulation of pentameric ligand-gated ion channels An emerging mechanistic perspective

机译：五聚体配体门控离子通道的变构调节机制的新兴机制。

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Pentameric ligand-gated ion channels (pLGICs) play a central role in intercellular communications in the nervous system by converting the binding of a chemical messenger-a neurotransmitter-into an ion flux through the postsynaptic membrane. They are oligomeric assemblies that provide prototypical examples of allosterically regulated integral membrane proteins. Here, we present an overview of the most recent advances on the signal transduction mechanism based on the X-ray structures of both prokaryotic and invertebrate eukaryotic pLGICs and atomistic Molecular Dynamics simulations. The present results suggest that ion gating involves a large structural reorganization of the molecule mediated by two distinct quaternary transitions, a global twisting and the blooming of the extracellular domain, which can be modulated by ligand binding at the topographically distinct orthosteric and allosteric sites. The emerging model of gating is consistent with a wealth of functional studies and will boost the development of novel pharmacological strategies.
机译：五聚体配体门控离子通道（pLGICs）通过将化学信使（一种神经递质）的结合转换为通过突触后膜的离子通量，在神经系统的细胞间通讯中发挥重要作用。它们是寡聚组装体，提供了变构调节的整合膜蛋白的典型例子。在这里，我们概述了基于原核和无脊椎动物真核pLGIC的X射线结构以及原子分子动力学模拟的信号转导机制的最新进展。目前的结果表明，离子门控涉及两个不同的四级过渡，整体扭曲和细胞外结构域的开花介导的分子的大结构重组，这可以通过在地形上不同的正构和变构位点的配体结合来调节。新兴的门控模型与大量的功能研究一致，并将促进新型药理学策略的发展。

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