Department of Pharmacy, Children's Hospital of Fudan University, National Children's Medical Center, Shanghai, 201102, China.
Department of Pharmacy, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, 430022, China.
Acta Pharmacol Sin. 2023 Jan;44(1):19-31. doi: 10.1038/s41401-022-00944-0. Epub 2022 Jul 15.
Inflammatory bowel disease (IBD) is a global health burden whose existing treatment is largely dependent on anti-inflammatory agents. Despite showing some therapeutic actions, their clinical efficacy and adverse events are unacceptable. Resolution as an active and orchestrated phase of inflammation involves improper inflammatory response with three key triggers, specialized pro-resolving mediators (SPMs), neutrophils and phagocyte efferocytosis. The formyl peptide receptor 2 (FPR2/ALX) is a human G protein-coupled receptor capable of binding SPMs and participates in the resolution process. This receptor has been implicated in several inflammatory diseases and its association with mouse model of IBD was established in some resolution-related studies. Here, we give an overview of three reported FPR2/ALX agonists highlighting their respective roles in pro-resolving strategies.
炎症性肠病 (IBD) 是全球健康负担,其现有治疗方法在很大程度上依赖于抗炎药物。尽管这些药物显示出一定的治疗作用,但它们的临床疗效和不良反应是不可接受的。消退是炎症的一个积极和协调的阶段,涉及到三个关键触发因素,即不当的炎症反应、特异性促解决介质 (SPM)、中性粒细胞和吞噬细胞凋亡。甲酰肽受体 2 (FPR2/ALX) 是一种能够结合 SPM 的人类 G 蛋白偶联受体,参与消退过程。该受体与多种炎症性疾病有关,其与 IBD 小鼠模型的关联在一些与消退相关的研究中得到了证实。在这里,我们概述了三种已报道的 FPR2/ALX 激动剂,重点介绍了它们在促解决策略中的各自作用。