Peptide toxins and small-molecule blockers of BK channels

doi:10.1038/aps.2015.139

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	Peptide toxins and small-molecule blockers of BK channels
	Yu, Mu 1; Liu, San-ling 1; Sun, Pei-bei 2; Pan, Hao 2; Tian, Chang-lin 1,2; Zhang, Long-hua 2
	2016
发表期刊	ACTA PHARMACOLOGICA SINICA
摘要	Large conductance, Ca2+-activated potassium (BK) channels play important roles in the regulation of neuronal excitability and the control of smooth muscle contractions. BK channels can be activated by changes in both the membrane potential and intracellular Ca2+ concentrations. Here, we provide an overview of the structural and pharmacological properties of BK channel blockers. First, the properties of different venom peptide toxins from scorpions and snakes are described, with a focus on their characteristic structural motifs, including their disulfide bond formation pattern, the binding interface between the toxin and BK channel, and the functional consequence of the blockage of BK channels by these toxins. Then, some representative non-peptide blockers of BK channels are also described, including their molecular formula and pharmacological effects on BK channels. The detailed categorization and descriptions of these BK channel blockers will provide mechanistic insights into the blockade of BK channels. The structures of peptide toxins and non-peptide compounds could provide templates for the design of new channel blockers, and facilitate the optimization of lead compounds for further therapeutic applications in neurological disorders or cardiovascular diseases.
文章类型	Review
关键词	Bk Channel Peptide Toxins Scorpion Venom Iberiotoxin Small-molecule Blockers Alkaloids
WOS标题词	Science & Technology ; Physical Sciences ; Life Sciences & Biomedicine
DOI	10.1038/aps.2015.139
关键词[WOS]	ACTIVATED POTASSIUM CHANNELS ; CA-2+-ACTIVATED K+ CHANNEL ; SCORPION BUTHUS-MARTENSI ; HUV-EC-C ; LARGE-CONDUCTANCE ; SMOOTH-MUSCLE ; CHARYBDOTOXIN BLOCK ; 3-DIMENSIONAL STRUCTURE ; FUNCTIONAL EXPRESSION ; ENDOTHELIAL-CELLS
收录类别	SCI
语种	英语
项目资助者	National Natural Science Foundation of China(31100847) ; National Natural Science Foundation of China(31100847) ; National Natural Science Foundation of China(31100847) ; National Natural Science Foundation of China(31100847) ; National Natural Science Foundation of China(31100847) ; National Natural Science Foundation of China(31100847) ; National Natural Science Foundation of China(31100847) ; National Natural Science Foundation of China(31100847) ; Youth Innovation Promotion Association CAS(2012323) ; Youth Innovation Promotion Association CAS(2012323) ; Youth Innovation Promotion Association CAS(2012323) ; Youth Innovation Promotion Association CAS(2012323) ; Youth Innovation Promotion Association CAS(2012323) ; Youth Innovation Promotion Association CAS(2012323) ; Youth Innovation Promotion Association CAS(2012323) ; Youth Innovation Promotion Association CAS(2012323) ; Fundamental Research Funds for Central Universities of China(WK2070000033) ; Fundamental Research Funds for Central Universities of China(WK2070000033) ; Fundamental Research Funds for Central Universities of China(WK2070000033) ; Fundamental Research Funds for Central Universities of China(WK2070000033) ; Fundamental Research Funds for Central Universities of China(WK2070000033) ; Fundamental Research Funds for Central Universities of China(WK2070000033) ; Fundamental Research Funds for Central Universities of China(WK2070000033) ; Fundamental Research Funds for Central Universities of China(WK2070000033) ; Specialized Research Fund for Doctoral Program of Higher Education(20113402110058) ; Specialized Research Fund for Doctoral Program of Higher Education(20113402110058) ; Specialized Research Fund for Doctoral Program of Higher Education(20113402110058) ; Specialized Research Fund for Doctoral Program of Higher Education(20113402110058) ; Specialized Research Fund for Doctoral Program of Higher Education(20113402110058) ; Specialized Research Fund for Doctoral Program of Higher Education(20113402110058) ; Specialized Research Fund for Doctoral Program of Higher Education(20113402110058) ; Specialized Research Fund for Doctoral Program of Higher Education(20113402110058)
WOS研究方向	Chemistry ; Pharmacology & Pharmacy
WOS类目	Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
WOS记录号	WOS:000367514700008
引用统计	被引频次：31[WOS] [WOS记录] [WOS相关记录]
文献类型	期刊论文
条目标识符	http://ir.hfcas.ac.cn:8080/handle/334002/22220
专题	中科院强磁场科学中心
作者单位	1.Chinese Acad Sci, High Field Magnet Lab, Hefei 230031, Peoples R China 2.Univ Sci & Technol China, Sch Life Sci, Hefei 230027, Peoples R China
第一作者单位	中科院强磁场科学中心
推荐引用方式 GB/T 7714	Yu, Mu,Liu, San-ling,Sun, Pei-bei,et al. Peptide toxins and small-molecule blockers of BK channels[J]. ACTA PHARMACOLOGICA SINICA,2016,37(1):56-66.
APA	Yu, Mu,Liu, San-ling,Sun, Pei-bei,Pan, Hao,Tian, Chang-lin,&Zhang, Long-hua.(2016).Peptide toxins and small-molecule blockers of BK channels.ACTA PHARMACOLOGICA SINICA,37(1),56-66.
MLA	Yu, Mu,et al."Peptide toxins and small-molecule blockers of BK channels".ACTA PHARMACOLOGICA SINICA 37.1(2016):56-66.

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文件名称/大小	文献类型	版本类型	开放类型	使用许可
Peptide toxins and s（1302KB）	期刊论文	作者接受稿	开放获取	CC BY-NC-SA	浏览下载