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Mar. Drugs 2017, 15(10), 295; https://doi.org/10.3390/md15100295

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

1
Department of Biology and Evolution of Marine Organisms, Stazione Zoologica Anton Dohrn, Villa Comunale, 80121 Naples, Italy
2
Department of Sciences, University of Basilicata, 75100 Potenza, Italy
*
Author to whom correspondence should be addressed.
Received: 28 July 2017 / Revised: 12 September 2017 / Accepted: 20 September 2017 / Published: 22 September 2017
(This article belongs to the Special Issue Marine Drugs and Ion Currents)
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Abstract

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. View Full-Text
Keywords: conotoxin; µ-conotoxin; ion current; sodium channel; pain transmission conotoxin; µ-conotoxin; ion current; sodium channel; pain transmission
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Tosti, E.; Boni, R.; Gallo, A. µ-Conotoxins Modulating Sodium Currents in Pain Perception and Transmission: A Therapeutic Potential. Mar. Drugs 2017, 15, 295.

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