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Cloning, expression and identification of KTX-Sp4, a selective Kv1.3 peptidic blocker from Scorpiops pococki
Zou,Yan1; Zhang,Feng1; Li,Yaxian1; Wang,Yuanfang1; Li,Yi1; Long,Zhengtao1; Shi,Shujuan1; Shuai,Li1,3; Liu,Jiukai1,3; Di,Zhiyong2; Yin,Shijin1,3
2017-11-06
发表期刊Cell & Bioscience
ISSN2045-3701
卷号7期号:1
摘要AbstractBackgroundSpecific and selective peptidic blockers of Kv1.3 channels can serve as a valuable drug lead for treating T cell-mediated autoimmune diseases, and scorpion venom is an important source of kv1.3 channel inhibitors. Through conducting transcriptomic sequencing for the venom gland of Scorpiops pococki from Xizang province of China, this research aims to discover a novel functional gene encoding peptidic blocker of Kv1.3, and identify its function.ResultsWe screened out a new peptide toxin KTX-Sp4 which had 43 amino acids including six cysteine residues. Electrophysiological experiments indicated that recombinant expression?products of KTX-Sp4 blocked both endogenous and exogenous Kv1.3 channel concentration-dependently, and exhibited good selectivity on Kv1.3 over Kv1.1, Kv1.2, respectively. Mutation experiments showed that the Kv1 turret region was responsible for the selectivity of KTX-Sp4 peptide on Kv1.3 over Kv1.1.ConclusionsThis work not only provided a novel lead compound for the development of anti autoimmune disease drugs, but also enriched the molecular basis for the interaction between scorpion toxins and potassium channels, serving as an important theoretical basis for designing high selective Kv1.3 peptide inhibitors.
关键词Peptide KTX-Sp4 Scorpiops pococki Kv1.3 Channel turret Selectivity
DOI10.1186/s13578-017-0187-x
语种英语
WOS记录号BMC:10.1186/s13578-017-0187-x
出版者BioMed Central
引用统计
文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/61834
专题中国科学院昆明植物研究所
通讯作者Di,Zhiyong; Yin,Shijin
作者单位1.
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GB/T 7714
Zou,Yan,Zhang,Feng,Li,Yaxian,et al. Cloning, expression and identification of KTX-Sp4, a selective Kv1.3 peptidic blocker from Scorpiops pococki[J]. Cell & Bioscience,2017,7(1).
APA Zou,Yan.,Zhang,Feng.,Li,Yaxian.,Wang,Yuanfang.,Li,Yi.,...&Yin,Shijin.(2017).Cloning, expression and identification of KTX-Sp4, a selective Kv1.3 peptidic blocker from Scorpiops pococki.Cell & Bioscience,7(1).
MLA Zou,Yan,et al."Cloning, expression and identification of KTX-Sp4, a selective Kv1.3 peptidic blocker from Scorpiops pococki".Cell & Bioscience 7.1(2017).
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