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Mar. Drugs 2010, 8(4), 1373-1393; doi:10.3390/md8041373
Review

The Outer Vestibule of the Na+ Channel–Toxin Receptor and Modulator of Permeation as Well as Gating

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Received: 3 February 2010 / Revised: 31 March 2010 / Accepted: 19 April 2010 / Published: 21 April 2010
(This article belongs to the Special Issue Tetrodotoxin)
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Abstract

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.
Keywords: tetrodotoxin; saxitoxin; sodium channel; use-dependent block; rate-dependent block; outer vestibule tetrodotoxin; saxitoxin; sodium channel; use-dependent block; rate-dependent block; outer vestibule
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Cervenka, R.; Zarrabi, T.; Lukacs, P.; Todt, H. The Outer Vestibule of the Na+ Channel–Toxin Receptor and Modulator of Permeation as Well as Gating. Mar. Drugs 2010, 8, 1373-1393.

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