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首页> 外文期刊>Biochemistry >Crotonic Acid Blocks the Gloeobacter Ligand-Gated Ion Channel (GLIC) via the Extracellular Domain
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Crotonic Acid Blocks the Gloeobacter Ligand-Gated Ion Channel (GLIC) via the Extracellular Domain

机译：巴豆酸通过细胞外结构域阻断gloeobacter配体门离子通道（GLIC）

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摘要

Cys-loop receptors play important roles in signal transduction in multicellular organisms, but similar proteins exist in prokaryotes, the best studied of-whit:his the Gloeobacter ligand-gated ion channel (GLIC). GLIC is activated by protons with 50% activation (pH(50)) at pH 5.5, and while a histidine residue in its pore-forming alpha-helix (M2) is known to be involved in gating, there is also evidence of a proton-sensitive region in the extracellular domain. However, this proton-sensitive region does not appear to be located in the region of GLIC equivalent to the agonist binding site in related proteins. Here we explore functional effects of a range of compounds that could bind to this site and show that some GABA analogues, the most potent of which is crotonic acid, inhibit GLIC function. Mutagenesis and docking studies suggest crotonic acid can bind to this region of the protein and, when bound, can. allosterically inhibit GLIC function. These data therefore suggest that there is a transduction pathway from the orthosteric binding site to the pore in GLIC, as exists in related eukaryotic ligand-gated ion channels, and thus provide further evidence that this prokaryotic receptor is a good model for understanding this family of proteins.
机译：半胱氨酸环受体在多细胞生物体的信号转导中起着重要作用，但是原核生物中存在类似的蛋白质，这是研究最好的白血球：其Gloeobacter配体门控离子通道（GLIC）。 GLIC在pH 5.5时被质子以50％的活化度（pH（50））活化，虽然已知其形成孔的α-螺旋（M2）中的组氨酸残基与门控有关，但也有质子的证据细胞外结构域中的敏感区域。然而，该质子敏感区似乎不位于​​与相关蛋白中激动剂结合位点等效的GLIC区域中。在这里，我们探索了可能与该位点结合的一系列化合物的功能效应，并表明某些GABA类似物（其中最有效的是巴豆酸）抑制了GLIC功能。诱变和对接研究表明，巴豆酸可以与蛋白质的这一区域结合，结合后可以。变构抑制GLIC功能。因此，这些数据表明，如相关真核配体门控离子通道中存在的那样，存在从正构结合位点到GLIC孔的转导途径，因此提供了进一步的证据，证明该原核受体是理解该家族的好模型。蛋白质。

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