Structure and function of ?-conotoxins, peptide-based sodium channel blockers with analgesic activity.
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SUBMITTER: Green BR
PROVIDER: S-EPMC4366142 | biostudies-literature | 2014 Oct
REPOSITORIES: biostudies-literature
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Structure and function of μ-conotoxins, peptide-based sodium channel blockers with analgesic activity.
Green Brad R BR Bulaj Grzegorz G Norton Raymond S RS
Future medicinal chemistry 20141001 15
μ-Conotoxins block voltage-gated sodium channels (VGSCs) and compete with tetrodotoxin for binding to the sodium conductance pore. Early efforts identified µ-conotoxins that preferentially blocked the skeletal muscle subtype (NaV1.4). However, the last decade witnessed a significant increase in the number of µ-conotoxins and the range of VGSC subtypes inhibited (NaV1.2, NaV1.3 or NaV1.7). Twenty µ-conotoxin sequences have been identified to date and structure-activity relationship studies of sev ...[more]
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