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• W2593688045 abstract "Local anesthetics, antiarrhythmics, and anticonvulsants include both charged and electroneutral compounds that block voltage-gated sodium channels. Prior studies have revealed a common drug-binding region within the pore, but details about the binding sites and mechanism of block remain unclear. Here, we use the x-ray structure of a prokaryotic sodium channel, NavMs, to model a eukaryotic channel and dock representative ligands. These include lidocaine, QX-314, cocaine, quinidine, lamotrigine, carbamazepine (CMZ), phenytoin, lacosamide, sipatrigine, and bisphenol A. Preliminary calculations demonstrated that a sodium ion near the selectivity filter attracts electroneutral CMZ but repels cationic lidocaine. Therefore, we further docked electroneutral and cationic drugs with and without a sodium ion, respectively. In our models, all the drugs interact with a phenylalanine in helix IVS6. Electroneutral drugs trap a sodium ion in the proximity of the selectivity filter, and this same site attracts the charged group of cationic ligands. At this position, even small drugs can block the permeation pathway by an electrostatic or steric mechanism. Our study proposes a common pharmacophore for these diverse drugs. It includes a cationic moiety and an aromatic moiety, which are usually linked by four bonds." @default.
• W2593688045 created "2017-03-16" @default.
• W2593688045 creator A5030029005 @default.
• W2593688045 creator A5088059071 @default.
• W2593688045 date "2017-03-03" @default.
• W2593688045 modified "2023-10-13" @default.
• W2593688045 title "Mechanism of sodium channel block by local anesthetics, antiarrhythmics, and anticonvulsants" @default.
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• W2593688045 doi "https://doi.org/10.1085/jgp.201611668" @default.
• W2593688045 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5379917" @default.
• W2593688045 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/28258204" @default.
• W2593688045 hasPublicationYear "2017" @default.
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