Institute of Pharmacology, Centre of Physiology and Pharmacology, Medical University of Vienna, 1090 Vienna, Austria.
Mar Drugs. 2010 Apr 21;8(4):1373-93. doi: 10.3390/md8041373.
The outer vestibule of voltage-gated Na(+) channels is formed by extracellular loops connecting the S5 and S6 segments of all four domains ("P-loops"), which fold back into the membrane. Classically, this structure has been implicated in the control of ion permeation and in toxin blockage. However, conformational changes of the outer vestibule may also result in alterations in gating, as suggested by several P-loop mutations that gave rise to gating changes. Moreover, partial pore block by mutated toxins may reverse gating changes induced by mutations. Therefore, toxins that bind to the outer vestibule can be used to modulate channel gating.
电压门控钠离子通道的外腔由连接所有四个结构域的 S5 和 S6 片段的细胞外环形成(“P 环”)，这些环折叠回膜内。传统上，这种结构被认为与离子渗透的控制和毒素阻断有关。然而，外腔的构象变化也可能导致门控的改变，这是由几个导致门控改变的 P 环突变所提示的。此外，突变毒素的部分孔隙阻断可能会逆转由突变引起的门控改变。因此，结合在外腔的毒素可用于调节通道门控。
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