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Voltage-Gated Sodium Channel Inhibition by µ-Conotoxins

Authors :
Kirsten L. McMahon
Irina Vetter
Christina I. Schroeder
Source :
Toxins, Vol 16, Iss 1, p 55 (2024)
Publication Year :
2024
Publisher :
MDPI AG, 2024.

Abstract

µ-Conotoxins are small, potent pore-blocker inhibitors of voltage-gated sodium (NaV) channels, which have been identified as pharmacological probes and putative leads for analgesic development. A limiting factor in their therapeutic development has been their promiscuity for different NaV channel subtypes, which can lead to undesirable side-effects. This review will focus on four areas of µ-conotoxin research: (1) mapping the interactions of µ-conotoxins with different NaV channel subtypes, (2) µ-conotoxin structure–activity relationship studies, (3) observed species selectivity of µ-conotoxins and (4) the effects of µ-conotoxin disulfide connectivity on activity. Our aim is to provide a clear overview of the current status of µ-conotoxin research.

Details

Language :
English
ISSN :
20726651
Volume :
16
Issue :
1
Database :
Directory of Open Access Journals
Journal :
Toxins
Publication Type :
Academic Journal
Accession number :
edsdoj.26cd559e85ab4274bb8dcdf46263cf5d
Document Type :
article
Full Text :
https://doi.org/10.3390/toxins16010055