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

页码：1424 / 1430

页数：7

共 40 条

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[29] A novel toxin variant from the Androctonus australis hector scorpion venom selectively activates Kv7.4 channel
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[30] A Potent and Selective Peptide Blocker of the Kv1.3 Channel: Prediction from Free-Energy Simulations and Experimental Confirmation
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