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

Eur J Med Chem. 2021 Mar 5:213:113167. doi: 10.1016/j.ejmech.2021.113167.

Monika Maciuszek ¹, Antonino Cacace ², Eoin Brennan ², Catherine Godson ², Timothy M Chapman ³

Affiliations

1 LifeArc, Accelerator Building, Open Innovation Campus, Stevenage, United Kingdom; The William Harvey Research Institute, Barts and The London School of Medicine, Queen Mary University of London, London, United Kingdom. Electronic address: maciuszekmonika@gmail.com.
2 Diabetes Complications Research Centre, Conway Institute & School of Medicine, University College Dublin, Dublin, Ireland.
3 LifeArc, Accelerator Building, Open Innovation Campus, Stevenage, United Kingdom.

PMID: 33486199 DOI: 10.1016/j.ejmech.2021.113167

Abstract

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.

Keywords

Agonists; FPR2/ALX; Inflammation; Resolution.

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