G蛋白偶联受体激酶在心血管疾病中的作用  

Role of G protein-coupled receptor kinases in cardiovascular diseases

作　　者：田艳君[1] 刘海青[2] 陈京[3] 白波[3] 

机构地区：[1]曲阜师范大学,山东曲阜273165 [2]泰山医学院,山东泰安271000 [3]济宁医学院,山东济宁272000

出　　处：《中国病理生理杂志》2013年第7期1327-1331,共5页Chinese Journal of Pathophysiology

基　　金：国家自然科学基金资助项目(No.30971081;No.31271243;No.81070961;No.81241052);山东省自然科学基金资助项目(No.ZR2009DZ004;No.ZR2011CM027;No.2012GSF11806);泰山学者建设专项资金

摘　　要：G蛋白偶联受体（G-protein-coupled receptors,GPCRs）是与G蛋白偶联的膜受体,也是目前已知最大的细胞膜受体家族。GPCRs能够被不同配体所激活,可将激素、神经递质、药物、趋化因子以及光线等多种化学性和物理性细胞外信号转导入细胞内,在多种生理活动和病理过程中发挥重要的调节作用。GPCRs被认为是高血压、心力衰竭、帕金森氏综合症等多种疾病的药物治疗靶点,市售药物约50%都是以GPCRs为靶点的[1]。G-protein-coupled receptors（GPCRs） are hitherto the largest family of membrane receptors.They activate associated heterotrimeric G-proteins and participate in the regulation of intracellular signaling pathways,which are accomplished via ligand binding to them.G-protein-coupled receptor kinases（GRKs） are key modulators of GPCR signaling.GRKs,in concert with β-arrestins,classically lead to desensitization and internalization of GPCR,thus preventing hyperactivation of GPCR second messenger cascades.Changes in the GRKs expression and regulation have featured prominently in many cardiovascular diseases,including heart failure,myocardial infarction,cardiac hypertrophy,and hypertension.Intensively studying the role of GRKs in cardiovascular diseases contributes to expounding the mechanism of correlated diseases.Herein,we review the role of GRKs in cardiovascular pathophysiology.

关 键 词：G蛋白偶联受体激酶 心血管疾病 

分 类 号：R363[医药卫生—病理学]