OdK2, a Kv1.3 channel-selective toxin from the venom of the Iranian scorpion Odonthobuthus doriae

被引：27
|
作者：
Abdel-Mottaleb, Yousra [1 ]
Vandendriessche, Thomas [1 ]
Clynen, Elke [2 ]
Landuyt, Bart [2 ]
Jalali, Amir [3 ]
Vatanpour, Hossein [4 ]
Schoofs, Liliane [2 ]
Tytgat, Jan [1 ]
机构：
[1] Univ Leuven, Toxicol Lab, B-3000 Leuven, Belgium
[2] Univ Leuven, Res Grp Funct Genom & Prote, B-3000 Leuven, Belgium
[3] Ahvaz Jundishapur Univ Med Sci, Dept Pharmacol & Toxicol, Ahvaz, Iran
[4] Shahid Beheshti Univ Med Sci, Dept Pharmacol & Toxicol, Tehran, Iran
来源：
TOXICON | 2008年 / 51卷 / 08期
关键词：
Odonthobuthus doriae; voltage-gated potassium channels; OdK2; alpha-KTX3.11; quadrupole ion cyclotron resonance; Fourier-transform mass spectrometry (QICR FT MS); multiple sclerosis;
D O I：
10.1016/j.toxicon.2008.03.027
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
The first Kv1.3 channel-selective toxin from the venom of the Iranian scorpion Odonthobuthus doriae (OdK2) was purified, sequenced and characterized physiologically. OdK2 consists of 38 amino acids, including six conserved cysteine and a C-terminal lysine residue, as revealed by the unique use of a quadrupole ion cyclotron resonance Fourier-transform mass spectrometer. Based on multiple sequence alignments, OdK2 was classified as alpha-KTX3.11. The pharmacological effects of OdK2 were studied on a panel of eight different cloned K+ channels (vertebrate Kv1.1-Kv1.6, Shaker IR and hERG) expressed in Xenopus laevis oocytes. Interestingly, OdK2 selectively inhibits the currents through Kv1.3 channels with an IC50 value of 7.2 +/- 2.7 nM. (c) 2008 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1424 / 1430
页数：7
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