中国科技核心期刊
CN:31-1600/Q
ISSN:1004-0374
“健康与疾病的免疫”国际学术研讨会通知      关于有网站冒充本刊网站的声明
《生命科学》 2016, 28(9): 965-977
KCNQ钾通道及其小分子调节剂研究进展
刘 妮1,2,吕 伟1,南发俊1,2*
(1 华东师范大学化学与分子工程学院,上海 200062;2 中国科学院上海药物研究所国家新药筛选中心,上海 201203)
摘 要:KCNQ 钾通道是一类电压门控钾离子通道,具有慢激活和不失活的特点,参与调控细胞的正常代谢。KCNQ 钾通道包括KCNQ1~KCNQ5 五个亚型,在心脏、神经元和平滑肌等组织广泛分布,并在调节细胞兴奋性和离子平衡中发挥着重要的生理功能。KCNQ 功能失调导致多种人类疾病,因此被认为是治疗癫痫、心律失常、疼痛、耳聋和认知功能障碍等疾病的重要药物靶点。2011 年,FDa 批准KCNQ 激动剂Retigabine 上市,进一步促进了以KCNQ 为靶点的小分子调节剂的研究。在综述中主要介绍了KCNQ 钾通道小分子调节剂的研究进展。
 
KCNQ potassium channel and the development of its small molecule modulators
LIU Ni1,2, LÜ Wei1, Nan Fa-Jun1,2*
(1 College of Chemistry and Molecular Engineering, East China Normal University, Shanghai 200062, China; 2 Chinese National Center for Drug Screening, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China)
Abstract: KCNQ channel belongs to voltage-gated potassium channel, characterised by a slow activation and deactivation current, and can regulate the normal metabolism process. KCNQ genes encode five KCNQ channel subunits (KCNQ1-5). Mutations in the KCNQ gene cause dysfunction in KCNQ channel, which leads to LQT1, DFNA2, epilepsy, pain and cognitived impairment etc. Therofore, KCNQ channel can be a therapeutic target to treat the related diseases. In 2011, FDA approved Retigabine for the adjunctive treatment of partial-onset seizures in patients with further promoting the research progress of KCNQ channel modulators. This review mainly introduces the development of KCNQ channel small molecule modulators.
 
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