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ACS Chem Neurosci. 2016 Oct 19;7(10):1463-1468. Epub 2016 Aug 8.

Inhibition of Sodium Ion Channel Function with Truncated Forms of Batrachotoxin.

Author information

1
Department of Chemistry, Stanford University , Stanford, California 94305-5080, United States.

Abstract

A novel family of small molecule inhibitors of voltage-gated sodium channels (NaVs) based on the structure of batrachotoxin (BTX), a well-known channel agonist, is described. Protein mutagenesis and electrophysiology experiments reveal the binding site as the inner pore region of the channel, analogous to BTX, alkaloid toxins, and local anesthetics. Homology modeling of the eukaryotic channel based on recent crystallographic analyses of bacterial NaVs suggests a mechanism of action for ion conduction block.

KEYWORDS:

SAR; Site II; batrachotoxin; electrophysiology; protein mutagenesis; sodium channel

PMID:
27501251
PMCID:
PMC5555364
DOI:
10.1021/acschemneuro.6b00212
[Indexed for MEDLINE]
Free PMC Article

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