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Molecules 2010, 15(4), 2825-2844; doi:10.3390/molecules15042825

µ-Conotoxins as Leads in the Development of New Analgesics

Walter and Eliza Hall Institute of Medical Research, Parkville, Victoria 3052, Australia
Received: 9 March 2010 / Revised: 6 April 2010 / Accepted: 12 April 2010 / Published: 19 April 2010
(This article belongs to the Special Issue Toxins - Organic and Analytical Chemistry)
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Voltage-gated sodium channels (VGSCs) contain a specific binding site for a family of cone shell toxins known as µ-conotoxins. As some VGSCs are involved in pain perception and µ-conotoxins are able to block these channels, µ-conotoxins show considerable potential as analgesics. Recent studies have advanced our understanding of the three-dimensional structures and structure-function relationships of the µ-conotoxins, including their interaction with VGSCs. Truncated peptide analogues of the native toxins have been created in which secondary structure elements are stabilized by non-native linkers such as lactam bridges. Ultimately, it would be desirable to capture the favourable analgesic properties of the native toxins, in particular their potency and channel sub-type selectivity, in non-peptide mimetics. Such mimetics would constitute lead compounds in the development of new therapeutics for the treatment of pain.
Keywords: cone shell; toxin; sodium channel; pain; peptide mimetic cone shell; toxin; sodium channel; pain; peptide mimetic
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Norton, R.S. µ-Conotoxins as Leads in the Development of New Analgesics. Molecules 2010, 15, 2825-2844.

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