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Structure-Function and Therapeutic Potential of Spider Venom-Derived Cysteine Knot Peptides Targeting Sodium Channels.
Front Pharmacol. 2019; 10:366.FP

Abstract

Spider venom-derived cysteine knot peptides are a mega-diverse class of molecules that exhibit unique pharmacological properties to modulate key membrane protein targets. Voltage-gated sodium channels (NaV) are often targeted by these peptides to allosterically promote opening or closing of the channel by binding to structural domains outside the channel pore. These effects can result in modified pain responses, muscle paralysis, cardiac arrest, priapism, and numbness. Although such effects are often deleterious, subtype selective spider venom peptides are showing potential to treat a range of neurological disorders, including chronic pain and epilepsy. This review examines the structure-activity relationships of cysteine knot peptides from spider venoms that modulate NaV and discusses their potential as leads to novel therapies for neurological disorders.

Authors+Show Affiliations

Centre for Pain Research, Institute for Molecular Bioscience, The University of Queensland, St Lucia, QLD, Australia.Centre for Pain Research, Institute for Molecular Bioscience, The University of Queensland, St Lucia, QLD, Australia.

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

31031623

Citation

Cardoso, Fernanda C., and Richard J. Lewis. "Structure-Function and Therapeutic Potential of Spider Venom-Derived Cysteine Knot Peptides Targeting Sodium Channels." Frontiers in Pharmacology, vol. 10, 2019, p. 366.
Cardoso FC, Lewis RJ. Structure-Function and Therapeutic Potential of Spider Venom-Derived Cysteine Knot Peptides Targeting Sodium Channels. Frontiers in pharmacology. 2019;10:366.
Cardoso, F. C., & Lewis, R. J. (2019). Structure-Function and Therapeutic Potential of Spider Venom-Derived Cysteine Knot Peptides Targeting Sodium Channels. Frontiers in Pharmacology, 10, 366. https://doi.org/10.3389/fphar.2019.00366
Cardoso FC, Lewis RJ. Structure-Function and Therapeutic Potential of Spider Venom-Derived Cysteine Knot Peptides Targeting Sodium Channels. Frontiers in pharmacology. 2019;10:366. PubMed PMID: 31031623.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Structure-Function and Therapeutic Potential of Spider Venom-Derived Cysteine Knot Peptides Targeting Sodium Channels. AU - Cardoso,Fernanda C, AU - Lewis,Richard J, Y1 - 2019/04/11/ PY - 2019/02/08/received PY - 2019/03/25/accepted PY - 2019/4/30/entrez PY - 2019/4/30/pubmed PY - 2019/4/30/medline KW - ICK peptides KW - novel drugs KW - spider venoms KW - structure–activity relationship KW - voltage-gated ion channels SP - 366 EP - 366 JF - Frontiers in pharmacology VL - 10 N2 - Spider venom-derived cysteine knot peptides are a mega-diverse class of molecules that exhibit unique pharmacological properties to modulate key membrane protein targets. Voltage-gated sodium channels (NaV) are often targeted by these peptides to allosterically promote opening or closing of the channel by binding to structural domains outside the channel pore. These effects can result in modified pain responses, muscle paralysis, cardiac arrest, priapism, and numbness. Although such effects are often deleterious, subtype selective spider venom peptides are showing potential to treat a range of neurological disorders, including chronic pain and epilepsy. This review examines the structure-activity relationships of cysteine knot peptides from spider venoms that modulate NaV and discusses their potential as leads to novel therapies for neurological disorders. SN - 1663-9812 UR - https://www.unboundmedicine.com/medline/citation/31031623/Structure_Function_and_Therapeutic_Potential_of_Spider_Venom_Derived_Cysteine_Knot_Peptides_Targeting_Sodium_Channels_ L2 - https://doi.org/10.3389/fphar.2019.00366 DB - PRIME DP - Unbound Medicine ER -
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