µ-conotoxins as leads in the development of new analgesics

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ID: 242576
2010
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Abstract
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.
Reference Key
norton2010molecules-conotoxins Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors ;Raymond S. Norton
Journal Journal of ethnopharmacology
Year 2010
DOI
10.3390/molecules15042825
URL
http://www.mdpi.com/1420-3049/15/4/2825/
Keywords
pain toxin peptide mimeticorganic chemistry

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