Interaction site for the inhibition of tarantula Jingzhaotoxin-XI on voltage-gated potassium channel Kv2.1

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成果类型：

期刊论文

作者：

Tao, Huai*（陶怀）;Chen, Xia;Deng, Meichun;Xiao, Yucheng;Wu, Yuanyuan;...

通讯作者：

Tao, Huai（陶怀）;Liang, Songping

作者机构：

[Tao, Huai; Zhou, Sainan; He, Yingchun] Hunan Univ Chinese Med, Dept Biochem & Mol Biol, Changsha 410208, Hunan, Peoples R China.

[Wu, Yuanyuan; Liu, Zhonghua; Liang, Songping; Xiao, Yucheng] Hunan Normal Univ, Coll Life Sci, Minist Educ, Key Lab Prot Chem & Dev Biol, Changsha 410081, Hunan, Peoples R China.

[Chen, Xia] Cent S Univ, Xiangya Hosp 2, Dept Orthoped, Changsha 410011, Hunan, Peoples R China.

[Tao, Huai; He, Yingchun] Hunan Univ Chinese Med, Div Stem Cell Regulat & Applicat, Changsha 410208, Hunan, Peoples R China.

[Deng, Meichun] Cent S Univ, State Key Lab Med Genet, Changsha 410013, Hunan, Peoples R China.

通讯机构：

[Tao, Huai; Liang, Songping] H

Hunan Univ Chinese Med, Dept Biochem & Mol Biol, Changsha 410208, Hunan, Peoples R China.

Hunan Normal Univ, Coll Life Sci, Minist Educ, Key Lab Prot Chem & Dev Biol, Changsha 410081, Hunan, Peoples R China.

语种：

英文

关键词：

Jingzhaotoxin-XI;Kv2.1;Mutation;Molecular determinant

期刊：

Toxicon

ISSN：

0041-0101

年：

2016

卷：

124

页码：

8-14

DOI：

10.1016/j.toxicon.2016.10.019

基金类别：

National 973 Project of ChinaNational Basic Research Program of China [2010CB529801]; National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [81503276, 31672290, 81573721, 81302953]; Hunan Provincial Education DepartmentHunan Provincial Education Department [15C1044]; Research Foundation of Stem Cell Regulation and Application of Hunan University of Chinese Medicine [2013GXB01]; Scientific Research Starting Foundation of Hunan University of Chinese Medicine [9982-1001-010]; Cooperative Innovation Center of Engineering and New Products for Developmental Biology of Hunan Province [20134486]; Natural Science Foundation of Hunan ProvinceNatural Science Foundation of Hunan Province [2016JJ3180]

机构署名：

本校为第一且通讯机构

院系归属：

医学院

中医学院

药学院

摘要：

Jingzhaotoxin-XI (JZTX-XI) is a 34-residue peptide from the Chinese tarantula Chilobrachys jingzhao venom that potently inhibits both voltage-gated sodium channel Nav1.5 and voltage-gated potassium channel Kv2.1. In the present study, we further showed that JZTX-XI blocked Kv2.1 currents with the 1050 value of 0.39 +/- 0.06 M. JZTX-XI significantly shifted the current-voltage (I V) curves and normalized conductance-voltage (G V) curves of Kv2.1 channel to more depolarized voltages. Ala-scanning mutagenesis analyses demonstrated that mutants 1273A, F274A, and E277A reduced toxin binding affinit...

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Interaction site for the inhibition of tarantula Jingzhaotoxin-XI on voltage-gated potassium channel Kv2.1

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