Voltage-Gated Sodium Channel Inhibition by μ-Conotoxins

被引：5
作者：
Mcmahon, Kirsten L. [1 ]
Vetter, Irina [1 ,2 ]
Schroeder, Christina I. [1 ,3 ]
机构：
[1] Univ Queensland, Inst Mol Biosci, Brisbane, Qld 4072, Australia
[2] Univ Queensland, Sch Pharm, Woolloongabba, Qld 4102, Australia
[3] Genentech Inc, 1 DNA Way, South San Francisco, CA 94080 USA
来源：
TOXINS | 2024年 / 16卷 / 01期
基金：
英国医学研究理事会;
关键词：
mu-conotoxin; peptide; structure-activity relationships; venom peptide; disulfide-rich peptide; voltage-gated sodium channels; subtype selectivity; SKELETAL-MUSCLE; MOLECULAR DETERMINANTS; DISULFIDE-BOND; CONUS-STRIATUS; POTENT INHIBITOR; PEPTIDE BLOCKER; GIIIA; KIIIA; TETRODOTOXIN; BINDING;
D O I：
10.3390/toxins16010055
中图分类号：
TS2 [食品工业];
学科分类号：
0832 ;
摘要：
mu-Conotoxins are small, potent pore-blocker inhibitors of voltage-gated sodium (Na-V) channels, which have been identified as pharmacological probes and putative leads for analgesic development. A limiting factor in their therapeutic development has been their promiscuity for different Na-V channel subtypes, which can lead to undesirable side-effects. This review will focus on four areas of mu-conotoxin research: (1) mapping the interactions of mu-conotoxins with different Na-V channel subtypes, (2) mu-conotoxin structure-activity relationship studies, (3) observed species selectivity of mu-conotoxins and (4) the effects of mu-conotoxin disulfide connectivity on activity. Our aim is to provide a clear overview of the current status of mu-conotoxin research.
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页数：17
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