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长链游离脂肪酸受体靶点药物研究进展

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

long-chain free fatty acidsperoxisome proliferator-activated receptorsGPR40GPR120drug development

张小春、赵妍妍、张丽君、梁向艳、赵玉峰

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西安医学院基础医学研究所,西安 710021

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

西安医学院科技创新团队项目

2021TD01

2024

中国新药杂志
中国医药科技出版社 中国医药集团总公司 中国药学会

中国新药杂志

CSTPCD北大核心
影响因子:1.039
ISSN:1003-3734
年,卷(期):2024.33(11)