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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, H;Liang, SP
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.
[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, H ; Liang, SP ] 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;*Molecular determinant;*Mutation
期刊:
Toxicon
ISSN:
0041-0101
年:
2016
卷:
124
页码:
8-14
基金类别:
National 973 Project of China#&#&#2010CB529801 National Natural Science Foundation of China#&#&#81503276#&#&#31672290#&#&#81573721#&#&#81302953 Scientific Research Fund of Hunan 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 Province#&#&#2016JJ3180
机构署名:
本校为其他机构
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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