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作 者:于曼曼 杨立莉 李棋芬 司继刚[2] YU Manman;YANG Lili;LI Qifen;SI Jigang(School of Pharmacy,Binzhou Medical College,Yantai,Shandong Province,264003 China;Department of Clinical Pharmacy,Zibo Central Hospital,Zibo,Shandong Province,255036 China)
机构地区:[1]滨州医学院药学院,山东烟台264003 [2]淄博市中心医院临床药学科,山东淄博255036
出 处:《系统医学》2022年第24期187-192,共6页Systems Medicine
基 金:山东省淄博市重点研发计划(2020ZC010112)。
摘 要:原发性高血压是多种心脑血管疾病的重要危险因素,会损害心、脑、肾等重要脏器,最终导致器官功能的衰竭。G蛋白偶联受体(G protein-coupled receptors,GPCRs)是真核生物中最大且种类最丰富的一类膜蛋白受体家族,介导了人体许多细胞信号通路,参与调节人体血压等正常生理功能。在GPCRs的信号转导过程中,G蛋白偶联受体激酶(G protein-coupled receptor kinases,GRKs)能够使活化的GPCR脱敏,终止其介导的信号转导通路,从而导致高血压的发生。在GRK家族成员中,GRK4具有固有活性,在血压调控相关的组织和器官中均有表达,和高血压的发生有着密切关联。本文将从GRK4对血压的调控机制、GRK4基因多态性、GRK4和高血压药物基因组学等方面综述GRK4在高血压中的研究进展。Primary hypertension is an important risk factor for many cardiovascular and cerebrovascular diseases,which can damage the heart,brain,kidneys and other important organs and eventually lead to organ failure.G protein-coupled receptors(GPCRs)are the largest and most abundant family of membrane protein receptors in eukaryotes,mediating many cellular signaling pathways in the human body and participating in the regulation of normal physiological functions such as human blood pressure.During the signaling process of GPCRs,G protein-coupled receptor kinases(GRKs)can desensitize activated GPCRs and terminate their mediated signaling pathways,leading to the development of hypertension.Among the GRK family members,GRK4 is intrinsically active and expressed in tissues and organs related to blood pressure regulation,and is closely associated with the development of hypertension.In this paper,we will review the research progress of GRK4 in hypertension from the mechanism of GRK4 regulation of blood pressure,GRK4 gene polymorphism,GRK4 and hypertension pharmacogenomics.
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