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Spider-venom peptides that target voltage-gated sodium channels: pharmacological tools and potential therapeutic leads.
Toxicon. 2012 Sep 15; 60(4):478-91.T

Abstract

Voltage-gated sodium (Na(V)) channels play a central role in the propagation of action potentials in excitable cells in both humans and insects. Many venomous animals have therefore evolved toxins that modulate the activity of Na(V) channels in order to subdue their prey and deter predators. Spider venoms in particular are rich in Na(V) channel modulators, with one-third of all known ion channel toxins from spider venoms acting on Na(V) channels. Here we review the landscape of spider-venom peptides that have so far been described to target vertebrate or invertebrate Na(V) channels. These peptides fall into 12 distinct families based on their primary structure and cysteine scaffold. Some of these peptides have become useful pharmacological tools, while others have potential as therapeutic leads because they target specific Na(V) channel subtypes that are considered to be important analgesic targets. Spider venoms are conservatively predicted to contain more than 10 million bioactive peptides and so far only 0.01% of this diversity been characterised. Thus, it is likely that future research will reveal additional structural classes of spider-venom peptides that target Na(V) channels.

Authors+Show Affiliations

Institute for Molecular Bioscience, The University of Queensland, 306 Carmody Road, St. Lucia, QLD 4072, Australia.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't
Review

Language

eng

PubMed ID

22543187

Citation

Klint, Julie K., et al. "Spider-venom Peptides That Target Voltage-gated Sodium Channels: Pharmacological Tools and Potential Therapeutic Leads." Toxicon : Official Journal of the International Society On Toxinology, vol. 60, no. 4, 2012, pp. 478-91.
Klint JK, Senff S, Rupasinghe DB, et al. Spider-venom peptides that target voltage-gated sodium channels: pharmacological tools and potential therapeutic leads. Toxicon. 2012;60(4):478-91.
Klint, J. K., Senff, S., Rupasinghe, D. B., Er, S. Y., Herzig, V., Nicholson, G. M., & King, G. F. (2012). Spider-venom peptides that target voltage-gated sodium channels: pharmacological tools and potential therapeutic leads. Toxicon : Official Journal of the International Society On Toxinology, 60(4), 478-91. https://doi.org/10.1016/j.toxicon.2012.04.337
Klint JK, et al. Spider-venom Peptides That Target Voltage-gated Sodium Channels: Pharmacological Tools and Potential Therapeutic Leads. Toxicon. 2012 Sep 15;60(4):478-91. PubMed PMID: 22543187.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Spider-venom peptides that target voltage-gated sodium channels: pharmacological tools and potential therapeutic leads. AU - Klint,Julie K, AU - Senff,Sebastian, AU - Rupasinghe,Darshani B, AU - Er,Sing Yan, AU - Herzig,Volker, AU - Nicholson,Graham M, AU - King,Glenn F, Y1 - 2012/04/20/ PY - 2012/02/14/received PY - 2012/04/07/accepted PY - 2012/5/1/entrez PY - 2012/5/1/pubmed PY - 2012/11/8/medline SP - 478 EP - 91 JF - Toxicon : official journal of the International Society on Toxinology JO - Toxicon VL - 60 IS - 4 N2 - Voltage-gated sodium (Na(V)) channels play a central role in the propagation of action potentials in excitable cells in both humans and insects. Many venomous animals have therefore evolved toxins that modulate the activity of Na(V) channels in order to subdue their prey and deter predators. Spider venoms in particular are rich in Na(V) channel modulators, with one-third of all known ion channel toxins from spider venoms acting on Na(V) channels. Here we review the landscape of spider-venom peptides that have so far been described to target vertebrate or invertebrate Na(V) channels. These peptides fall into 12 distinct families based on their primary structure and cysteine scaffold. Some of these peptides have become useful pharmacological tools, while others have potential as therapeutic leads because they target specific Na(V) channel subtypes that are considered to be important analgesic targets. Spider venoms are conservatively predicted to contain more than 10 million bioactive peptides and so far only 0.01% of this diversity been characterised. Thus, it is likely that future research will reveal additional structural classes of spider-venom peptides that target Na(V) channels. SN - 1879-3150 UR - https://www.unboundmedicine.com/medline/citation/22543187/Spider_venom_peptides_that_target_voltage_gated_sodium_channels:_pharmacological_tools_and_potential_therapeutic_leads_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0041-0101(12)00444-8 DB - PRIME DP - Unbound Medicine ER -