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首页> 外文期刊>Acta crystallographica, Section D. Biological crystallography >Genuine open form of the pentameric ligand-gated ion channel GLIC
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Genuine open form of the pentameric ligand-gated ion channel GLIC

机译：五聚体配体门控离子通道GLIC的真正开放形式

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摘要

Pentameric ligand-gated ion channels (pLGICs) mediate fast chemical neurotransmission of nerve signalling in the central and peripheral nervous systems. GLIC is a bacterial homologue of eukaryotic pLGIC, the X-ray structure of which has been determined in three different conformations. GLIC is thus widely used as a model to study the activation and the allosteric transition of this family of receptors. The recently solved high-resolution structure of GLIC (2.4 angstrom resolution) in the active state revealed two bound acetate molecules in the extracellular domain (ECD). Here, it is shown that these two acetates exactly overlap with known sites of pharmacological importance in pLGICs, and their potential influence on the structure of the open state is studied in detail. Firstly, experimental evidence is presented for the correct assignment of these acetate molecules by using the anomalous dispersion signal of bromoacetate. Secondly, the crystal structure of GLIC in the absence of acetate was solved and it is shown that acetate binding induces local conformational changes that occur in strategic sites of the ECD. It is expected that this acetate-free structure will be useful in future computational studies of the gating transition in GLIC and other pLGICs.
机译：五聚体配体门控离子通道（pLGIC）介导中枢神经系统和周围神经系统中神经信号的快速化学神经传递。 GLIC是真核pLGIC的细菌同源物，其X射线结构已经以三种不同的构象确定。因此，GLIC被广泛用作研究该受体家族的激活和变构转变的模型。最近在活动状态下解析的GLIC高分辨率结构（分辨率为2.4埃）揭示了胞外域（ECD）中有两个结合的乙酸酯分子。在此显示，这两种乙酸盐与pLGIC中具有重要药理学意义的位点完全重叠，并且详细研究了它们对开放状态结构的潜在影响。首先，通过使用溴乙酸盐的异常分散信号，为正确分配这些乙酸盐分子提供了实验证据。其次，解决了在不存在乙酸盐的情况下GLIC的晶体结构，结果表明乙酸盐的结合诱导了在ECD关键部位发生的局部构象变化。预期这种无乙酸盐的结构将在将来的GLIC和其他pLGIC的门控转换的计算研究中有用。

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