The desensitization gate of inhibitory Cys-loop receptors.,Nature Communications

当前位置： X-MOL 学术 › Nat. Commun. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

The desensitization gate of inhibitory Cys-loop receptors.
Nature Communications ( IF 14.7 ) Pub Date : 2015-Apr-20 , DOI: 10.1038/ncomms7829
Marc Gielen ₁ , Philip Thomas ₁ , Trevor G Smart ₁

Affiliation

Cys-loop neurotransmitter-gated ion channels are vital for communication throughout the nervous system. Following activation, these receptors enter into a desensitized state in which the ion channel shuts even though the neurotransmitter molecules remain bound. To date, the molecular determinants underlying this most fundamental property of Cys-loop receptors have remained elusive. Here we present a generic mechanism for the desensitization of Cys-loop GABAA (GABAARs) and glycine receptors (GlyRs), which both mediate fast inhibitory synaptic transmission. Desensitization is regulated by interactions between the second and third transmembrane segments, which affect the ion channel lumen near its intracellular end. The GABAAR and GlyR pore blocker picrotoxin prevented desensitization, consistent with its deep channel-binding site overlapping a physical desensitization gate.

中文翻译：

抑制性 Cys 环受体的脱敏门。

Cys 环神经递质门控离子通道对于整个神经系统的通信至关重要。激活后，这些受体进入脱敏状态，即使神经递质分子保持结合，离子通道也会关闭。迄今为止，Cys 环受体这一最基本特性的分子决定因素仍然难以捉摸。在这里，我们提出了 Cys 环 GABAA (GABAARs) 和甘氨酸受体 (GlyRs) 脱敏的一般机制，它们都介导快速抑制性突触传递。脱敏受第二和第三跨膜段之间的相互作用调节，这会影响靠近其细胞内端的离子通道腔。GABAAR 和 GlyR 毛孔阻滞剂印防己毒素可防止脱敏，

更新日期：2015-04-24

点击分享查看原文

点击收藏

公开下载

阅读更多本刊新发论文本刊介绍/投稿指南