Wang Jiaying, Miao Zhishuo, Gao Yinhuang, Xie ZhiZhong, Liu Menghua, Zou Wei
School of Pharmacy, Hunan Provincial Maternal and Child Health Care Hospital, University of South China, Hengyang, 421001, China.
Key Laboratory of Drug Metabolism Research and Evaluation of the State Drug Administration, Guangdong Provincial Key Laboratory of New Drug Screening, School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China.
Pharmacol Rep. 2025 Jun;77(3):593-609. doi: 10.1007/s43440-025-00704-x. Epub 2025 Mar 18.
Formyl peptide receptor 2 (FPR2) is a G protein-coupled receptor with seven transmembrane domains, widely distributed in human cells. It plays a crucial role in inflammation-related diseases. Known for its "double-edged sword" nature, FPR2 can bind a variety of exogenous and endogenous ligands, mediating both pro-inflammatory and anti-inflammatory responses in tissues such as eyes, liver, joints, lungs, nerves, and blood vessels. FPR2's bioactivities are regulated by a complex network of genes and signaling pathways. However, the precise regulatory mechanisms governing its functions in different inflammatory conditions are still not well understood. This review summarizes the FPR2's activities in various inflammation-related diseases and looks into its potential as a therapeutic target. This review highlights recent advances in developing exogenous agonists for FPR2 and discusses receptor expression across species to support nonclinical research. Overall, this review aims to clarify FPR2's role in inflammation and provide insights for the development of new drugs against inflammatory diseases.
甲酰肽受体2(FPR2)是一种具有七个跨膜结构域的G蛋白偶联受体,广泛分布于人体细胞中。它在炎症相关疾病中起着至关重要的作用。FPR2以其“双刃剑”性质而闻名,它可以结合多种外源性和内源性配体,在眼睛、肝脏、关节、肺、神经和血管等组织中介导促炎和抗炎反应。FPR2的生物活性受复杂的基因和信号通路网络调控。然而,在不同炎症条件下控制其功能的精确调控机制仍未得到充分理解。本综述总结了FPR2在各种炎症相关疾病中的活性,并探讨了其作为治疗靶点的潜力。本综述重点介绍了开发FPR2外源性激动剂的最新进展,并讨论了跨物种的受体表达以支持非临床研究。总体而言,本综述旨在阐明FPR2在炎症中的作用,并为开发抗炎症疾病的新药提供见解。