针对阿尔茨海默病治疗的G蛋白偶联受体及其药物研究进展

G protein-coupled receptors and related drug development for Alzheimer's disease: research advances

G蛋白偶联受体(GPCR)作为体内最大的蛋白质超家族,通过结合和调节G蛋白活性,参与体内几乎所有的生理进程,成为多种药物的重要作用靶点。目前针对阿尔茨海默病的GPCR靶点通路和相关药理学研究尚比较缺乏,研究GPCR与阿尔茨海默病之间的关系,对于指导开发以GPCR为靶点的阿尔茨海默病治疗药物具有重要意义。本文综述了近几年阿尔茨海默病的GPCR靶点和相关药物研究进展,主要包括阿片受体、毒蕈碱型乙酰胆碱受体、5-羟色胺受体等,并对本课题组开展的相关研究作了概述。

As the largest superfamily of receptors,G protein-coupled receptors（GPCR） are involved in almost overall physiological function and pathological process via binding with G protein and regulating its activity.A variety of drugs are discovered specific to GPCR therapeutic targets.Until now,the research of GPCR pathways and related pharmacological progress associated with Alzheimer＇s disease is still deficient.Study of the relationship between GPCR and Alzheimer＇s disease established a guideline on development of GPCR-target therapeutic drugs.This review summarizes the GPCR and relevant drug development associated with Alzheimer＇s disease in recent years,including opioid receptors family,muscarinic based type acetylcholine receptors,serotonin receptors,etc,as well as our laboratory research status.