4.7 Review

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

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 213, Issue -, Pages -

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2021.113167

Keywords

FPR2/ALX; Agonists; Resolution; Inflammation

Funding

  1. European Union [675111]
  2. Marie Curie Actions (MSCA) [675111] Funding Source: Marie Curie Actions (MSCA)

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FPR2/ALX plays a crucial role in maintaining host defense and orchestrating the inflammatory process by responding to various agonists. These agonists include lipids, proteins, peptides, and synthetic small molecule agonists, which promote resolution and tissue regeneration during inflammation.
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.

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