Conotoxins targeting neuronal voltage-gated sodium channel subtypes: potential analgesics?

Knapp, Oliver, McArthur, Jeffrey R. and Adams, David J. (2012) Conotoxins targeting neuronal voltage-gated sodium channel subtypes: potential analgesics?. Toxins, 4 11: 1236-1260. doi:10.3390/toxins4111236


Author Knapp, Oliver
McArthur, Jeffrey R.
Adams, David J.
Title Conotoxins targeting neuronal voltage-gated sodium channel subtypes: potential analgesics?
Journal name Toxins   Check publisher's open access policy
ISSN 2072-6651
Publication date 2012-01-01
Sub-type Critical review of research, literature review, critical commentary
DOI 10.3390/toxins4111236
Open Access Status DOI
Volume 4
Issue 11
Start page 1236
End page 1260
Total pages 25
Place of publication Basel, Switzerland
Publisher M D P I AG
Language eng
Subject 3005 Toxicology
2307 Health, Toxicology and Mutagenesis
Abstract Voltage-gated sodium channels (VGSC) are the primary mediators of electrical signal amplification and propagation in excitable cells. VGSC subtypes are diverse, with different biophysical and pharmacological properties, and varied tissue distribution. Altered VGSC expression and/or increased VGSC activity in sensory neurons is characteristic of inflammatory and neuropathic pain states. Therefore, VGSC modulators could be used in prospective analgesic compounds. VGSCs have specific binding sites for four conotoxin families: μ-, μO-, δ- and ί-conotoxins. Various studies have identified that the binding site of these peptide toxins is restricted to well-defined areas or domains. To date, only the μ- and μO-family exhibit analgesic properties in animal pain models. This review will focus on conotoxins from the μ- and μO-families that act on neuronal VGSCs. Examples of how these conotoxins target various pharmacologically important neuronal ion channels, as well as potential problems with the development of drugs from conotoxins, will be discussed.
Keyword μ-conotoxin
μO-conotoxin
Analgesic
Nav1.3
Nav1.7
Nav1.8
Nav1.9
Nociception
Pain
voltage-gated sodium channel
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Non-UQ

Document type: Journal Article
Sub-type: Critical review of research, literature review, critical commentary
Collections: Queensland Brain Institute Publications
School of Biomedical Sciences Publications
 
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Created: Tue, 28 Oct 2014, 04:08:35 EST by Sylvie Pichelin on behalf of Queensland Brain Institute