Strategies for the Development of Conotoxins as New Therapeutic Leads

doi:10.3390/md11072293

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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

Ryan M. Brady, Jonathan B. Baell and Raymond S. Norton *

Monash Institute of Pharmaceutical Science, Monash University, 381 Royal Parade, Parkville 3052, Australia

* Author to whom correspondence should be addressed.

Received: 14 April 2013; in revised form: 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

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MDPI and ACS Style

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.

AMA Style

Brady RM, Baell JB, Norton RS. Strategies for the Development of Conotoxins as New Therapeutic Leads. Marine Drugs. 2013; 11(7):2293-2313.

Chicago/Turabian Style

Brady, Ryan M.; Baell, Jonathan B.; Norton, Raymond S. 2013. "Strategies for the Development of Conotoxins as New Therapeutic Leads." Mar. Drugs 11, no. 7: 2293-2313.

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