Characterization of a T-superfamily conotoxin TxVC from Conus textile that selectively targets neuronal nAChR subtypes

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	Characterization of a T-superfamily conotoxin TxVC from Conus textile that selectively targets neuronal nAChR subtypes
	Wang, Shuo 1; Du, Tianpeng 2; Liu, Zhuguo 1; Wang, Sheng 3; Wu, Ying 3; Ding, Jiuping 3; Jiang, Ling 2; Dai, Qiuyun 1
刊名	BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
	2014-11-07
卷号	454 期号:1 页码:151-156
关键词	Conus textile T-superfamily conotoxin TxVC Neuronal nicotinic acetylcholine receptor Selectivity NMR structure
英文摘要	T-superfamily conotoxins have a typical cysteine pattern of "CC-CC", and are known to mainly target calcium or sodium ion channels. Recently, we screened the targets of a series of T-superfamily conotoxins and found that a new T-superfamily conotoxin TxVC (KPCCSIHDNSCCGL-NH2) from the venom of Conus textile. It selectively targeted the neuronal nicotinic acetylcholine receptor (nAChR) subtypes alpha 4 beta 2 and alpha 3 beta 2, with IC50 values of 343.4 and 1047.2 nM, respectively, but did not exhibit obvious pharmacological effects on voltage-gated potassium, sodium or calcium channel in DRG cells, the BK channels expressed in HEK293 cells, or the Kv channels in L beta T2 cells. The changes in the inhibitory activities of its Ala mutants, the NMR structure, and molecular simulation results based on other conotoxins targeting nAChR alpha 4 beta 2, all demonstrated that the residues Ile(6) and Leu(14) were the main hydrophobic pharmacophores. To our best knowledge, this is the first T-superfamily conotoxin that inhibits neuronal nAChRs and possesses high binding affinity to alpha 4 beta 2. This finding will expand the knowledge of the targets of T-superfamily conotoxins and the motif information could help the design of new nAChR inhibitors. (C) 2014 Elsevier Inc. All rights reserved.
WOS标题词	Science & Technology ; Life Sciences & Biomedicine
类目[WOS]	Biochemistry & Molecular Biology ; Biophysics
研究领域[WOS]	Biochemistry & Molecular Biology ; Biophysics
关键词[WOS]	NICOTINIC ACETYLCHOLINE-RECEPTORS ; ALPHA-CONOTOXIN ; PEPTIDE ; VENOM ; IDENTIFICATION ; CONOPEPTIDE ; DIVERSITY
收录类别	SCI
语种	英语
WOS记录号	WOS:000346693500026
公开日期	2015-07-14
内容类型	期刊论文
源URL	[http://ir.wipm.ac.cn/handle/112942/1342]
专题	武汉物理与数学研究所_磁共振基础研究部
作者单位	1.Beijing Inst Biotechnol, Beijing 10071, Peoples R China 2.Chinese Acad Sci, Key Lab Magnet Resonance Biol Syst, State Key Lab Magnet Resonance & Atom & Mol Phys, Natl Ctr Magnet Resonance Wuhan,Wuhan Inst Phys &, Wuhan 430071, Peoples R China 3.Huazhong Univ Sci & Technol, Key Lab Mol Biophys, Minist Educ, Coll Life Sci & Technol, Wuhan 430074, Peoples R China
推荐引用方式 GB/T 7714	Wang, Shuo,Du, Tianpeng,Liu, Zhuguo,et al. Characterization of a T-superfamily conotoxin TxVC from Conus textile that selectively targets neuronal nAChR subtypes[J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,2014,454(1):151-156.
APA	Wang, Shuo.,Du, Tianpeng.,Liu, Zhuguo.,Wang, Sheng.,Wu, Ying.,...&Dai, Qiuyun.(2014).Characterization of a T-superfamily conotoxin TxVC from Conus textile that selectively targets neuronal nAChR subtypes.BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,454(1),151-156.
MLA	Wang, Shuo,et al."Characterization of a T-superfamily conotoxin TxVC from Conus textile that selectively targets neuronal nAChR subtypes".BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS 454.1(2014):151-156.