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近年来,作为具有多种治疗潜力的促解决剂,针对甲酰肽受体 2(FPR2/ALX)激动剂的设计和开发取得了新进展。

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

机构信息

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.

Diabetes Complications Research Centre, Conway Institute & School of Medicine, University College Dublin, Dublin, Ireland.

出版信息

Eur J Med Chem. 2021 Mar 5;213:113167. doi: 10.1016/j.ejmech.2021.113167. Epub 2021 Jan 12.

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.

摘要

在生理条件下,炎症反应的启动、持续时间和幅度受到严格调控,以确保体内平衡的恢复。在这些情况下,炎症的消退是由内源性产生的介质的反应决定的。对内源性介质的模拟是促进炎症消退治疗炎症性疾病的原则基础。甲酰肽受体 2(FPR2/ALX)是一种 G 蛋白偶联受体,已知在维持宿主防御和调节炎症过程中发挥着关键作用。FPR2/ALX 可以被广泛的不同激动剂激活,包括脂质、蛋白质、肽和一系列合成小分子激动剂。本综述的重点是提供一个关于开发促进解决和组织再生的 FPR2/ALX 激动剂的最新进展的全面概述。

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