| Peptide toxins and small-molecule blockers of BK channels | |
| Yu, Mu1; Liu, San-ling1; Sun, Pei-bei2; Pan, Hao2; Tian, Chang-lin1,2; Zhang, Long-hua2 | |
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 2016 | |
| 卷号 | 37期号:1页码:56-66 |
| 关键词 | Bk Channel Peptide Toxins Scorpion Venom Iberiotoxin Small-molecule Blockers Alkaloids |
| DOI | 10.1038/aps.2015.139 |
| 文献子类 | Review |
| 英文摘要 | 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. |
| WOS关键词 | 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 |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000367514700008 |
| 资助机构 | 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) ; 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) |
| 内容类型 | 期刊论文 |
| 源URL | [http://ir.hfcas.ac.cn:8080/handle/334002/22220]  |
| 专题 | 合肥物质科学研究院_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 |
| 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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