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

µ-Conotoxins as Leads in the Development of New Analgesics

Received: 9 March 2010; in revised form: 6 April 2010 / Accepted: 12 April 2010 / Published: 19 April 2010
(This article belongs to the Special Issue Toxins - Organic and Analytical Chemistry)
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.
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.
Keywords: cone shell; toxin; sodium channel; pain; peptide mimetic
PDF Full-text Download PDF Full-Text [503 KB, uploaded 18 June 2014 19:32 CEST]

Export to BibTeX |

MDPI and ACS Style

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

AMA Style

Norton RS. µ-Conotoxins as Leads in the Development of New Analgesics. Molecules. 2010; 15(4):2825-2844.

Chicago/Turabian Style

Norton, Raymond S. 2010. "µ-Conotoxins as Leads in the Development of New Analgesics." Molecules 15, no. 4: 2825-2844.

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert