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- Title
µ-Conotoxins as Leads in the Development of New Analgesics.
- Authors
Norton, Raymond S.
- 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.
- Subjects
SODIUM channels; PHYSIOLOGICAL transport of sodium; PEPTIDE synthesis; ANALGESICS; PAIN management; SENSES; ANTIBODY-toxin conjugates; BIOCHEMISTRY; CHEMICAL biology
- Publication
Molecules, 2010, Vol 15, Issue 4, p2825
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules15042825