A toxin to nervous, cardiac, and endocrine ERG K+ channels isolated from Centruroides noxius scorpion venom

被引:92
作者
Gurrola, GB
Rosati, B
Rocchetti, M
Pimienta, G
Zaza, A
Arcangeli, A
Olivotto, M
Possani, LD
Wanke, E
机构
[1] Univ Milan, Dipartimento Fisiol & Biochim Gen, I-20133 Milan, Italy
[2] Univ Milano Bicocca, Dept Biotechnol & Biosci, I-20126 Milan, Italy
[3] Univ Milan, Dept Gen Physiol & Biochem, Lab Electrophysiol, I-20133 Milan, Italy
[4] Natl Autonomous Univ Mexico, Inst Biotechnol, Dept Mol Recognit & Struct Biol, Cuernavaca 62271, Morelos, Mexico
[5] Univ Florence, Inst Gen Pathol, I-50134 Florence, Italy
关键词
eag gene family; erg gene; ergtoxin; scorpion toxin; action potential;
D O I
10.1096/fasebj.13.8.953
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Toxins isolated from a variety of venoms are tools for probing the physiological function and structure of ion channels. The ether-a-go-go-related genes (erg) codify for the K+ channels (ERG), which are crucial in neurons and are impaired in human long-QT syndrome and Drosophila 'seizure' mutants. We have isolated a peptide from the scorpion Centruroides noxius Hoffmann that has no sequence homologies with other toxins, and demonstrate that it specifically inhibits (IC50=16+/-1 nM) only ERG channels of different species and distinct histogenesis. These results open up the possibility of investigating ERG channel structure-function relationships and novel pharmacological tools with potential therapeutic efficacy.
引用
收藏
页码:953 / 962
页数:10
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