Voltage-Gated Sodium Channel Inhibition by µ-Conotoxins.

Toxins (Basel)

Institute for Molecular Biosciences, The University of Queensland, Brisbane, QLD 4072, Australia.

Published: January 2024

µ-Conotoxins are small, potent pore-blocker inhibitors of voltage-gated sodium (Na) 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 Na 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 Na 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.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10819908PMC
http://dx.doi.org/10.3390/toxins16010055DOI Listing

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