期刊
FUTURE MEDICINAL CHEMISTRY
卷 6, 期 15, 页码 1677-1698出版社
FUTURE SCI LTD
DOI: 10.4155/FMC.14.107
关键词
-
资金
- NHMRC
- National Institutes of General Medical Sciences, National Institutes of Health [GM48677]
mu-Conotoxins block voltage-gated sodium channels (VGSCs) and compete with tetrodotoxin for binding to the sodium conductance pore. Early efforts identified mu-conotoxins that preferentially blocked the skeletal muscle subtype (Na(V)1.4). However, the last decade witnessed a significant increase in the number of mu-conotoxins and the range of VGSC subtypes inhibited (Na(V)1.2, Na(V)1.3 or Na(V)1.7). Twenty mu-conotoxin sequences have been identified to date and structure-activity relationship studies of several of these identified key residues responsible for interactions with VGSC subtypes. Efforts to engineer-in subtype specificity are driven by in vivo analgesic and neuromuscular blocking activities. This review summarizes structural and pharmacological studies of mu-conotoxins, which show promise for development of selective blockers of Na(V)1.2, and perhaps also Na(V)1.1,1.3 or 1.7.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据