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Veratridine: A Janus-Faced Modulator of Voltage-Gated Sodium Ion Channels

Cite this: ACS Chem. Neurosci. 2020, 11, 3, 418-426
Publication Date (Web):January 17, 2020
https://doi.org/10.1021/acschemneuro.9b00621
Copyright © 2020 American Chemical Society
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Abstract

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Voltage-gated sodium ion channels (NaVs) are integral to both neuronal and muscular signaling and are a primary target for a number of proteinaceous and small molecule toxins. Included among these neurotoxins is veratridine (VTD), a C-nor-D homosteroidal alkaloid from the seeds of members of the Veratrum genus. VTD binds to NaV within the pore region, causing a hyperpolarizing shift in the activation threshold in addition to reducing peak current. We have characterized the activity of VTD against heterologously expressed rat NaV1.4 and have demonstrated that VTD acts on the channel as either an agonist or antagonist depending on the nature of the electrophysiological stimulation protocol. Structure–activity studies with VTD and VTD derivatives against NaV mutants show that the functional duality of VTD can be decoupled. These findings suggest that the dichotomous activity of VTD may derive from two distinct, use-dependent binding orientations of the toxin.

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  • NMR spectra of VTD derivatives, protein expression and PCR methods, electrophysiology recording data, computational modeling (PDF)

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