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µ-Conotoxins Modulating Sodium Currents in Pain Perception and Transmission: A Therapeutic Potential

The Conus genus includes around 500 species of marine mollusks with a peculiar production of venomous peptides known as conotoxins (CTX). Each species is able to produce up to 200 different biological active peptides. Common structure of CTX is the low number of amino acids stabilized by disulfide b...

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Autores principales: Tosti, Elisabetta, Boni, Raffaele, Gallo, Alessandra
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5666403/
https://www.ncbi.nlm.nih.gov/pubmed/28937587
http://dx.doi.org/10.3390/md15100295
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author Tosti, Elisabetta
Boni, Raffaele
Gallo, Alessandra
author_facet Tosti, Elisabetta
Boni, Raffaele
Gallo, Alessandra
author_sort Tosti, Elisabetta
collection PubMed
description The Conus genus includes around 500 species of marine mollusks with a peculiar production of venomous peptides known as conotoxins (CTX). Each species is able to produce up to 200 different biological active peptides. Common structure of CTX is the low number of amino acids stabilized by disulfide bridges and post-translational modifications that give rise to different isoforms. µ and µO-CTX are two isoforms that specifically target voltage-gated sodium channels. These, by inducing the entrance of sodium ions in the cell, modulate the neuronal excitability by depolarizing plasma membrane and propagating the action potential. Hyperexcitability and mutations of sodium channels are responsible for perception and transmission of inflammatory and neuropathic pain states. In this review, we describe the current knowledge of µ-CTX interacting with the different sodium channels subtypes, the mechanism of action and their potential therapeutic use as analgesic compounds in the clinical management of pain conditions.
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spelling pubmed-56664032017-11-09 µ-Conotoxins Modulating Sodium Currents in Pain Perception and Transmission: A Therapeutic Potential Tosti, Elisabetta Boni, Raffaele Gallo, Alessandra Mar Drugs Review The Conus genus includes around 500 species of marine mollusks with a peculiar production of venomous peptides known as conotoxins (CTX). Each species is able to produce up to 200 different biological active peptides. Common structure of CTX is the low number of amino acids stabilized by disulfide bridges and post-translational modifications that give rise to different isoforms. µ and µO-CTX are two isoforms that specifically target voltage-gated sodium channels. These, by inducing the entrance of sodium ions in the cell, modulate the neuronal excitability by depolarizing plasma membrane and propagating the action potential. Hyperexcitability and mutations of sodium channels are responsible for perception and transmission of inflammatory and neuropathic pain states. In this review, we describe the current knowledge of µ-CTX interacting with the different sodium channels subtypes, the mechanism of action and their potential therapeutic use as analgesic compounds in the clinical management of pain conditions. MDPI 2017-09-22 /pmc/articles/PMC5666403/ /pubmed/28937587 http://dx.doi.org/10.3390/md15100295 Text en © 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Review
Tosti, Elisabetta
Boni, Raffaele
Gallo, Alessandra
µ-Conotoxins Modulating Sodium Currents in Pain Perception and Transmission: A Therapeutic Potential
title µ-Conotoxins Modulating Sodium Currents in Pain Perception and Transmission: A Therapeutic Potential
title_full µ-Conotoxins Modulating Sodium Currents in Pain Perception and Transmission: A Therapeutic Potential
title_fullStr µ-Conotoxins Modulating Sodium Currents in Pain Perception and Transmission: A Therapeutic Potential
title_full_unstemmed µ-Conotoxins Modulating Sodium Currents in Pain Perception and Transmission: A Therapeutic Potential
title_short µ-Conotoxins Modulating Sodium Currents in Pain Perception and Transmission: A Therapeutic Potential
title_sort µ-conotoxins modulating sodium currents in pain perception and transmission: a therapeutic potential
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5666403/
https://www.ncbi.nlm.nih.gov/pubmed/28937587
http://dx.doi.org/10.3390/md15100295
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