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Mar. Drugs 2013, 11(7), 2293-2313; doi:10.3390/md11072293
Review

Strategies for the Development of Conotoxins as New Therapeutic Leads

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Received: 14 April 2013 / Revised: 27 May 2013 / Accepted: 6 June 2013 / Published: 28 June 2013
(This article belongs to the Special Issue Marine Peptides and Their Mimetics)
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Abstract

Peptide toxins typically bind to their target ion channels or receptors with high potency and selectivity, making them attractive leads for therapeutic development. In some cases the native peptide as it is found in the venom from which it originates can be used directly, but in many instances it is desirable to truncate and/or stabilize the peptide to improve its therapeutic properties. A complementary strategy is to display the key residues that make up the pharmacophore of the peptide toxin on a non-peptidic scaffold, thereby creating a peptidomimetic. This review exemplifies these approaches with peptide toxins from marine organisms, with a particular focus on conotoxins.
Keywords: peptide toxin; peptidomimetic; ion channel; pain; cone snail peptide toxin; peptidomimetic; ion channel; pain; cone snail
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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Brady, R.M.; Baell, J.B.; Norton, R.S. Strategies for the Development of Conotoxins as New Therapeutic Leads. Mar. Drugs 2013, 11, 2293-2313.

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