PURIFICATION AND CHARACTERIZATION OF 3 INHIBITORS OF VOLTAGE-DEPENDENT K+ CHANNELS FROM LEIURUS-QUINQUESTRIATUS VAR HEBRAEUS VENOM
PURIFICATION AND CHARACTERIZATION OF 3 INHIBITORS OF VOLTAGE-DEPENDENT K+ CHANNELS FROM LEIURUS-QUINQUESTRIATUS VAR HEBRAEUS VENOM
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DOI：
10.1021/bi00188a012
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发表时间：
1994-06-07
期刊：
影响因子：
2.9
通讯作者：
MACKINNON, R
中科院分区：
文献类型：
--
作者：
GARCIA, ML;GARCIACALVO, M;MACKINNON, R
本文报道了五纹蝎Leiurus quinquestriatus var. hebraeus是基于其阻断Shaker K+通道的能力而被鉴定的。这些毒素已经使用HPLC技术纯化，并通过质谱、氨基酸分析和序列测定表征为38个氨基酸的肽。通过使用重组方法产生全功能合成毒素来确认其化学身份。这些肽是Shaker K+通道（Kd < 1 nM）以及Shaker的哺乳动物同系物的有效抑制剂。它们与其他先前描述的K+通道毒素有关，但如果K+通道抑制剂来源于蝎毒，则在更大的家族中形成新的亚类。我们将这些毒素分别命名为agitoxin 1、2和3。
Three new toxins from the venom of the scorpion Leiurus quinquestriatus var. hebraeus have been identified on the basis of their ability to block the Shaker K+ channel. These toxins have been purified using HPLC techniques and characterized as 38 amino acid peptides by mass spectroscopy, amino acid analysis, and sequence determination. Their chemical identity was confirmed by producing fully functional synthetic toxins using recombinant methods. These peptides are potent inhibitors of the Shaker K+ channel (K-d < 1 nM) as well as the mammalian homologues of Shaker. They are related to other previously described K+ channel toxins, but form a new subclass within the larger family if K+ channel inhibitors derived from scorpion venom. We have named these toxins agitoxin 1, 2, and 3, respectively.