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Review

Voltage-Gated Sodium Channel Inhibition by µ-Conotoxins

by
Kirsten L. McMahon
1,
Irina Vetter
1,2,* and
Christina I. Schroeder
1,3,*
1
Institute for Molecular Biosciences, The University of Queensland, Brisbane, QLD 4072, Australia
2
The School of Pharmacy, The University of Queensland, Woolloongabba, QLD 4102, Australia
3
Genentech, 1 DNA Way, South San Francisco, CA 94080, USA
*
Authors to whom correspondence should be addressed.
Toxins 2024, 16(1), 55; https://doi.org/10.3390/toxins16010055
Submission received: 21 November 2023 / Revised: 10 January 2024 / Accepted: 11 January 2024 / Published: 18 January 2024
(This article belongs to the Special Issue Conotoxins: Evolution, Classifications and Targets)

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.
Keywords: µ-conotoxin; peptide; structure–activity relationships; venom peptide; disulfide-rich peptide; voltage-gated sodium channels; subtype selectivity µ-conotoxin; peptide; structure–activity relationships; venom peptide; disulfide-rich peptide; voltage-gated sodium channels; subtype selectivity

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MDPI and ACS Style

McMahon, K.L.; Vetter, I.; Schroeder, C.I. Voltage-Gated Sodium Channel Inhibition by µ-Conotoxins. Toxins 2024, 16, 55. https://doi.org/10.3390/toxins16010055

AMA Style

McMahon KL, Vetter I, Schroeder CI. Voltage-Gated Sodium Channel Inhibition by µ-Conotoxins. Toxins. 2024; 16(1):55. https://doi.org/10.3390/toxins16010055

Chicago/Turabian Style

McMahon, Kirsten L., Irina Vetter, and Christina I. Schroeder. 2024. "Voltage-Gated Sodium Channel Inhibition by µ-Conotoxins" Toxins 16, no. 1: 55. https://doi.org/10.3390/toxins16010055

APA Style

McMahon, K. L., Vetter, I., & Schroeder, C. I. (2024). Voltage-Gated Sodium Channel Inhibition by µ-Conotoxins. Toxins, 16(1), 55. https://doi.org/10.3390/toxins16010055

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