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Review ArticleReview Article

Conus Venom Peptide Pharmacology

Richard J. Lewis, Sébastien Dutertre, Irina Vetter and MacDonald J. Christie
Annette C. Dolphin, ASSOCIATE EDITOR
Pharmacological Reviews April 2012, 64 (2) 259-298; DOI: https://doi.org/10.1124/pr.111.005322
Richard J. Lewis
Institute for Molecular Bioscience, the University of Queensland in St. Lucia, Brisbane, Queensland, Australia (R.J.L., S.D., I.V.); and Discipline of Pharmacology, the University of Sydney, Sydney, New South Wales, Australia (M.J.C.)
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Sébastien Dutertre
Institute for Molecular Bioscience, the University of Queensland in St. Lucia, Brisbane, Queensland, Australia (R.J.L., S.D., I.V.); and Discipline of Pharmacology, the University of Sydney, Sydney, New South Wales, Australia (M.J.C.)
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Irina Vetter
Institute for Molecular Bioscience, the University of Queensland in St. Lucia, Brisbane, Queensland, Australia (R.J.L., S.D., I.V.); and Discipline of Pharmacology, the University of Sydney, Sydney, New South Wales, Australia (M.J.C.)
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MacDonald J. Christie
Institute for Molecular Bioscience, the University of Queensland in St. Lucia, Brisbane, Queensland, Australia (R.J.L., S.D., I.V.); and Discipline of Pharmacology, the University of Sydney, Sydney, New South Wales, Australia (M.J.C.)
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Annette C. Dolphin
Institute for Molecular Bioscience, the University of Queensland in St. Lucia, Brisbane, Queensland, Australia (R.J.L., S.D., I.V.); and Discipline of Pharmacology, the University of Sydney, Sydney, New South Wales, Australia (M.J.C.)
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Abstract

Conopeptides are a diverse group of recently evolved venom peptides used for prey capture and/or defense. Each species of cone snails produces in excess of 1000 conopeptides, with those pharmacologically characterized (∼0.1%) targeting a diverse range of membrane proteins typically with high potency and specificity. The majority of conopeptides inhibit voltage- or ligand-gated ion channels, providing valuable research tools for the dissection of the role played by specific ion channels in excitable cells. It is noteworthy that many of these targets are found to be expressed in pain pathways, with several conopeptides having entered the clinic as potential treatments for pain [e.g., pyroglutamate1-MrIA (Xen2174)] and one now marketed for intrathecal treatment of severe pain [ziconotide (Prialt)]. This review discusses the diversity, pharmacology, structure-activity relationships, and therapeutic potential of cone snail venom peptide families acting at voltage-gated ion channels (ω-, μ-, μO-, δ-, ι-, and κ-conotoxins), ligand-gated ion channels (α-conotoxins, σ-conotoxin, ikot-ikot, and conantokins), G-protein-coupled receptors (ρ-conopeptides, conopressins, and contulakins), and neurotransmitter transporters (χ-conopeptides), with expanded discussion on the clinical potential of sodium and calcium channel inhibitors and α-conotoxins. Expanding the discovery of new bioactives using proteomic/transcriptomic approaches combined with high-throughput platforms and better defining conopeptide structure-activity relationships using relevant membrane protein crystal structures are expected to grow the already significant impact conopeptides have had as both research probes and leads to new therapies.

Footnotes

  • This work was supported by a National Health and Medical Research Council of Australia (NHMRC) Research Fellowship (to R.J.L., M.J.C.); an NHMRC Trainee Fellowship (to I.V.), a University of Queensland Postdoctoral Fellowship (to S.D.), and an NHMRC Program Grant (to R.J.L., M.J.C.).

  • This article is available online at http://pharmrev.aspetjournals.org.

    http://dx.doi.org/10.1124/pr.111.005322.

  • © 2012 by The American Society for Pharmacology and Experimental Therapeutics
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Pharmacological Reviews: 64 (2)
Pharmacological Reviews
Vol. 64, Issue 2
1 Apr 2012
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Review ArticleReview Article

CONOPEPTIDE PHARMACOLOGY

Richard J. Lewis, Sébastien Dutertre, Irina Vetter and MacDonald J. Christie
Pharmacological Reviews April 1, 2012, 64 (2) 259-298; DOI: https://doi.org/10.1124/pr.111.005322

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Review ArticleReview Article

CONOPEPTIDE PHARMACOLOGY

Richard J. Lewis, Sébastien Dutertre, Irina Vetter and MacDonald J. Christie
Pharmacological Reviews April 1, 2012, 64 (2) 259-298; DOI: https://doi.org/10.1124/pr.111.005322
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  • Article
    • Abstract
    • I. Introduction
    • II. ω-Conotoxin Inhibitors of Voltage-Gated Calcium Channels
    • II. Conotoxins Interacting with Voltage-Gated Sodium Channels
    • III. κ-Conotoxins Interacting with Potassium Channels
    • IV. Conotoxins Interacting with Ligand-Gated Ion Channels
    • V. Conotoxins Interacting with G Protein-Coupled Receptors and Neurotransmitter Transporters
    • VI. Conclusions and Outlook
    • Acknowledgments
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