长链游离脂肪酸受体靶点药物研究进展  

Research progress on the development of drugs targeting receptors of long-chain free fatty acids

作　　者：张小春 赵妍妍 张丽君 梁向艳 赵玉峰[1] ZHANG Xiao-chun;ZHAO Yan-yan;ZHANG Li-jun;LIANG Xiang-yan;ZHAO Yu-feng(Institute of Basic Medical Science,Xi'an Medical University,Xi'an 710021,China)

机构地区：[1]西安医学院基础医学研究所,西安710021

出　　处：《中国新药杂志》2024年第11期1121-1125,共5页Chinese Journal of New Drugs

基　　金：西安医学院科技创新团队项目(2021TD01)。

摘　　要：长链游离脂肪酸(long-chain free fatty acids,LCFFA)不仅是机体的能量物质,而且作为配体可激活相应受体发挥作用。LCFFA受体包括过氧化物酶体增殖物激活受体等核受体和G-蛋白偶联细胞膜受体GPR40及GPR120,在机体物质能量代谢和免疫功能调节等方面起着重要作用,成为近年备受关注的药物靶点。以LCFFA受体为靶点的药物研发进展迅速,多个新的化合物依次进入临床前和临床研究,有些已应用于临床。本文对此领域的药物研发情况进行综述,旨在为进一步的药物研究和开发提供参考。Long-chain free fatty acids(LCFFA)are not only the metabolic fuel for the body but also the ligands to activate cellular receptors.LCFFA receptors include the nuclear receptors(peroxisome proliferator-activated receptor-α,-β/δ,and-γ)and G protein-coupled cell membrane receptors(GPR40 and GPR120).Both of them play an important role in the regulation of energy metabolism and immune function.LCFFA receptors have been recognized as drug targets for decades.The research and development of drugs targeting LCFFA receptors is progressing rapidly.Many new compounds have entered preclinical and clinical research,some of which have been applied in clinic.Herein,the progress on the development of drugs targeting LCFFA receptors is summarized to provide reference for deeper research and drug development.

关 键 词：长链游离脂肪酸 过氧化物酶体增殖物激活受体 GPR40 GPR120 药物研发 

分 类 号：R962[医药卫生—药理学]