Garcia M L, Garcia-Calvo M, Hidalgo P, Lee A, MacKinnon R
Department of Membrane Biochemistry and Biophysics, Merck Research Laboratories, Rahway, New Jersey 07065.
Biochemistry. 1994 Jun 7;33(22):6834-9. doi: 10.1021/bi00188a012.
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 (Kd < 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 of K+ channel inhibitors derived from scorpion venom. We have named these toxins agitoxin 1, 2, and 3, respectively.
基于对以色列金蝎毒液中三种新毒素阻断Shaker钾通道的能力，已对其进行了鉴定。这些毒素已通过高效液相色谱（HPLC）技术纯化，并通过质谱分析、氨基酸分析和序列测定确定为38个氨基酸的肽。通过重组方法制备出具有完全功能的合成毒素，从而证实了它们的化学结构。这些肽是Shaker钾通道（解离常数Kd<1 nM）以及Shaker的哺乳动物同源物的强效抑制剂。它们与其他先前描述的钾通道毒素相关，但在源自蝎毒的钾通道抑制剂大家族中形成了一个新的亚类。我们分别将这些毒素命名为激动毒素1、2和3。
