鼠源甲酰肽受体 2 的抗炎作用:配体特异性对白细胞反应和实验性炎症的影响。
Anti-inflammatory role of the murine formyl-peptide receptor 2: ligand-specific effects on leukocyte responses and experimental inflammation.
机构信息
The William Harvey Research Institute, Barts and The London School of Medicine, Queen Mary University of London.
Medical Research Council Centre for Inflammation, Edinburgh, United Kingdom.
出版信息
J Immunol. 2010 Mar 1;184(5):2611-2619. doi: 10.4049/jimmunol.0903526. Epub 2010 Jan 27.
The human formyl-peptide receptor (FPR)-2 is a G protein-coupled receptor that transduces signals from lipoxin A(4), annexin A1, and serum amyloid A (SAA) to regulate inflammation. In this study, we report the creation of a novel mouse colony in which the murine FprL1 FPR2 homologue, Fpr2, has been deleted and describe its use to explore the biology of this receptor. Deletion of murine fpr2 was verified by Southern blot analysis and PCR, and the functional absence of the G protein-coupled receptor was confirmed by radioligand binding assays. In vitro, Fpr2(-/-) macrophages had a diminished response to formyl-Met-Leu-Phe itself and did not respond to SAA-induced chemotaxis. ERK phosphorylation triggered by SAA was unchanged, but that induced by the annexin A1-derived peptide Ac2-26 or other Fpr2 ligands, such as W-peptide and compound 43, was attenuated markedly. In vivo, the antimigratory properties of compound 43, lipoxin A(4), annexin A1, and dexamethasone were reduced notably in Fpr2(-/-) mice compared with those in wild-type littermates. In contrast, SAA stimulated neutrophil recruitment, but the promigratory effect was lost following Fpr2 deletion. Inflammation was more marked in Fpr2(-/-) mice, with a pronounced increase in cell adherence and emigration in the mesenteric microcirculation after an ischemia-reperfusion insult and an augmented acute response to carrageenan-induced paw edema, compared with that in wild-type controls. Finally, Fpr2(-/-) mice exhibited higher sensitivity to arthrogenic serum and were completely unable to resolve this chronic pathology. We conclude that Fpr2 is an anti-inflammatory receptor that serves varied regulatory functions during the host defense response. These data support the development of Fpr2 agonists as novel anti-inflammatory therapeutics.
人源甲酰肽受体(FPR)-2 是一种 G 蛋白偶联受体,它能将内源性配体脂氧素 A(4)、膜联蛋白 A1 和血清淀粉样蛋白 A(SAA)的信号转导,从而调控炎症反应。本研究报告了一种新型小鼠品系的建立,该品系中鼠源 FprL1/FPR2 同源物 Fpr2 已被敲除,并描述了该品系用于探索该受体生物学功能的应用。通过 Southern blot 分析和 PCR 验证了鼠源 Fpr2 的缺失,放射性配体结合试验证实了 G 蛋白偶联受体的功能缺失。体外研究显示,Fpr2(-/-) 型巨噬细胞对甲酰基-Met-Leu-Phe 本身的反应减弱,并且对 SAA 诱导的趋化性无反应。SAA 诱导的 ERK 磷酸化没有改变,但 Annexin A1 衍生肽 Ac2-26 或其他 Fpr2 配体(如 W-肽和化合物 43)诱导的 ERK 磷酸化明显减弱。体内研究显示,与野生型同窝仔鼠相比,Fpr2(-/-) 型小鼠中化合物 43、脂氧素 A(4)、膜联蛋白 A1 和地塞米松的抗趋化作用明显减弱。相反,SAA 刺激中性粒细胞募集,但 Fpr2 缺失后这种趋化作用丧失。Fpr2(-/-) 型小鼠炎症反应更为明显,缺血再灌注损伤后肠系膜微循环中细胞黏附和迁移明显增加,角叉菜胶诱导的爪肿胀急性反应增强,与野生型对照组相比差异显著。最后,Fpr2(-/-) 型小鼠对关节炎血清更为敏感,并且完全不能缓解这种慢性病理。我们的结论是,Fpr2 是一种抗炎受体,在宿主防御反应中发挥多种调节功能。这些数据支持开发 Fpr2 激动剂作为新型抗炎治疗药物。