Recent advances in the design and development of formyl peptide receptor 2 (FPR2/ALX) agonists as pro-resolving agents with diverse therapeutic potential

被引：46

作者：

Maciuszek, Monika ^{[1
,2
]}

Cacace, Antonino ^{[3
,4
]}

Brennan, Eoin ^{[3
,4
]}

Godson, Catherine ^{[3
,4
]}

Chapman, Timothy M. ^{[1
]}

机构：

[1] LifeArc, Accelerator Bldg,Open Innovat Campus, Stevenage, Herts, England

[2] Queen Mary Univ London, Barts & London Sch Med, William Harvey Res Inst, London, England

[3] Univ Coll Dublin, Conway Inst, Diabet Complicat Res Ctr, Dublin, Ireland

[4] Univ Coll Dublin, Sch Med, Dublin, Ireland

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2021年 / 213卷

关键词：

FPR2/ALX; Agonists; Resolution; Inflammation;

D O I：

10.1016/j.ejmech.2021.113167

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Under physiological conditions the initiation, duration and amplitude of inflammatory responses are tightly regulated to ensure the restoration of homeostasis. The resolution of inflammation in these circumstances is dictated by responses to endogenously generated mediators. Mimicry of such mediators underpins the principle of promoting the resolution of inflammation in treating inflammatory pathologies. The formyl peptide receptor 2 (FPR2/ALX) is a G-protein coupled receptor known to play a crucial role in maintaining host defence and orchestrating the inflammatory process. FPR2/ALX can be activated by a wide range of distinct agonists, including lipids, proteins, peptides, and an array of synthetic small molecule agonists. The focus of this review is to provide a comprehensive overview of recent progress made in the development of FPR2/ALX agonists which promote resolution and tissue regeneration. (C) 2021 The Authors. Published by Elsevier Masson SAS.

引用

页数：23

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[121] Lipoxin A4 modifies platelet-derived growth factor-induced profibrotic gene expression in human renal mesangial cells [J].