Strategies for the development of conotoxins as new therapeutic leads

Research output: Contribution to journalArticleResearchpeer-review

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.
Original languageEnglish
Pages (from-to)2293 - 2313
Number of pages21
JournalMarine Drugs
Volume11
Issue number7
DOIs
Publication statusPublished - 2013

Cite this

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author = "Ryan Brady and Baell, {Jonathan Bayldon} and Norton, {Raymond Stanley}",
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Strategies for the development of conotoxins as new therapeutic leads. / Brady, Ryan; Baell, Jonathan Bayldon; Norton, Raymond Stanley.

In: Marine Drugs, Vol. 11, No. 7, 2013, p. 2293 - 2313.

Research output: Contribution to journalArticleResearchpeer-review

TY - JOUR

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AU - Norton, Raymond Stanley

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N2 - 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.

AB - 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.

UR - http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3736424/pdf/marinedrugs-11-02293.pdf

U2 - 10.3390/md11072293

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M3 - Article

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SP - 2293

EP - 2313

JO - Marine Drugs

JF - Marine Drugs

SN - 1660-3397

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