Abstract
Small conductance Ca2+-activated potassium (SK) channels play a key role in the regulation of neuronal excitability. Positive modulation of potassium ion channels has been suggested as a potential therapeutic strategy to normalize the excitability of neurons, in movement disorders such as ataxia and Amyotrophic Lateral Sclerosis (ALS). Riluzole is the only FDA approved drug for ALS, although its therapeutic effects are only modest. Riluzole positively modulates SK channels, which contributes to its neuroprotective effects. With crystallography, we discovered the binding pocket of riluzole in SK2 channels. This binding pocket was further validated through combined techniques including site directed mutagenesis and electrophysiological recordings. These data suggest that the binding pocket identified by crystallography is indeed the functional binding pocket through which riluzole exerts the positive modulation of channel activity.
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