• Handb Exp Pharmacol · Jan 2014

    Review

    Probing gating mechanisms of sodium channels using pore blockers.

    • Marcel P Goldschen-Ohm and Baron Chanda.
    • Department of Neuroscience, University of Wisconsin, Madison, WI, USA.
    • Handb Exp Pharmacol. 2014 Jan 1;221:183-201.

    AbstractSeveral classes of small molecules and peptides bind at the central pore of voltage-gated sodium channels either from the extracellular or intracellular side of the membrane and block ion conduction through the pore. Biophysical studies that shed light on the chemical nature, accessibility, and kinetics of binding of these naturally occurring and synthetic compounds reveal a wealth of information about how these channels gate. Here, we discuss insights into the structural underpinnings of gating of the channel pore and its coupling to the voltage sensors obtained from pore blockers including site 1 neurotoxins and local anesthetics.

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