烟酸受体GPR109a及相关激动剂的研究进展

Research progress in nicotinic acid receptor GPR109a and related agonists

烟酸是临床应用几十年的降血脂药物,近年来研究发现,烟酸作用于G蛋白偶联受体109a(GPR109a)和GPR109b,该受体主要在脂肪细胞和多种免疫细胞中表达。烟酸受体的发现以及对相关不良反应作用机制的研究为寻找活性更强、不良反应较小的降脂药物开启了一条新的途径,为相关心血管疾病及糖尿病并发症的治疗提供了新的思路。本文对以GPR109a为靶标的药物研究成果进行综述。

Nicotinic acid（niacin） has been used for decades to treat dyslipidaemias. Recently ,the G protein- coupled receptor（GPCR） of niacin was found,including GPR109a and GPR109b ,which mainly express in adipocytes and immune cells. The discovery of the niacin receptor, which is coupled with a greater under- standing of the mechanism responsible for the side effects has therefore opened the door for the development of effective, tolerable drugs for the treatment of dyslipidaemia and the associated cardiovascular disease and diabetes. In this paper, research results of drugs based on GPR109a as target were reviewed.