摘要
电压门控钠离子通道是一类门控状态由细胞膜内外电势差所控制,仅在去极化膜电压下才能被激活打开的跨膜钠通道蛋白。其中,Nav1.4在骨骼肌中高度表达,主要形成肌膜动作电位上升支,参与人体一系列骨骼肌相关的生理病理活动。钠离子通道阻滞药与激活药是治疗心血管系统钠离子通道病的两大类药物,对其进行深入、全面的了解具有重要意义。本文从Nav1.4的分子结构、功能、药物开发等方面出发,对Nav1.4的调节机制、相关疾病以及高选择性药物研究情况进行简要综述,为基于Nav1.4作为靶标研发的药物奠定一定的理论依据。
Voltage-gated sodium channels are transmembrane sodium channel proteins whose gated state is controlled by the difference in electrical potential between the inside and outside of the cell membrane,and which can only be activated and opened by depolarising membrane voltage.Nav1.4 is highly expressed in a skeletal muscle and mainly forms the ascending action potential branch,which is involved in a range of skeletal muscle-related physiopathological action activities in the body.Sodium channel blockers and activators are two classes of drugs used to treat sodium channel disorders in the cardiovascular system,and it is important to have an in-depth and comprehensive understanding of them.In this paper,from the aspects of Nav1.4 molecular structure,function,drug development,and so on,the regulatory mechanism of Nav1.4,related diseases,and the research of highly selective drugs are briefly reviewed,which lays a certain theoretical basis for the development of drugs based on Nav1.4 as a target.
作者
刘欢
潘兰英
LIU Huan;PAN Lanying(Zhejiang Provincial Key Laboratory of Resources Protection and Innovation of Traditional Chinese Medicine,College of Food and Health,Zhejiang Agriculture and Forestry University,Hangzhou 311300,China;Shulan International Medical College,Zhejiang Shuren University,Hangzhou 310015,China)
出处
《生命的化学》
CAS
2023年第6期922-927,共6页
Chemistry of Life
基金
浙江省自然基金项目(LBY22H270002)
浙江省自然基金项目(LY20C040001)。
