Voltage gated sodium channels as drug discovery targets

Voltage-gated sodium (Na V ) channels are a family of transmembrane ion channel proteins. They function by forming a gated, water-filled pore to help establish and control cell membrane potential via control of the flow of ions between the intracellular and the extracellular environments. Blockade o...

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Bibliographic Details
Published in:Channels (Austin, Tex.) Tex.), 2015-11, Vol.9 (6), p.360-366
Main Authors: Bagal, Sharan K, Marron, Brian E, Owen, Robert M, Storer, R Ian, Swain, Nigel A
Format: Article
Language:English
Subjects:
Amino Acid Sequence
Analgesics - chemistry
Analgesics - pharmacology
Animals
Anti-Arrhythmia Agents - chemistry
Anti-Arrhythmia Agents - pharmacology
Anticonvulsants - chemistry
Anticonvulsants - pharmacology
Drug Discovery - methods
Humans
Molecular Sequence Data
Review
Sodium Channel Blockers - chemistry
Sodium Channel Blockers - pharmacology
sodium channel drugs
sodium channel structure
sodium channel toxins
Voltage-Gated Sodium Channels - metabolism
voltage-gated sodium channels Electrophysiology screening
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Summary:Voltage-gated sodium (Na V ) channels are a family of transmembrane ion channel proteins. They function by forming a gated, water-filled pore to help establish and control cell membrane potential via control of the flow of ions between the intracellular and the extracellular environments. Blockade of Na V s has been successfully accomplished in the clinic to enable control of pathological firing patterns that occur in a diverse range of conditions such as chronic pain, epilepsy, and cardiac arrhythmias. First generation sodium channel modulator drugs, despite low inherent subtype selectivity, preferentially act on over-excited cells which reduces undesirable side effects in the clinic. However, the limited therapeutic indices observed with the first generation demanded a new generation of sodium channel inhibitors. The structure, function and the state of the art in sodium channel modulator drug discovery are discussed in this chapter.
ISSN:1933-6950
1933-6969
DOI:10.1080/19336950.2015.1079674