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Formylpeptide 受体 2:命名、结构、信号转导和转化研究展望:国际药理学联合会药理学评论 35。

Formylpeptide receptor 2: Nomenclature, structure, signalling and translational perspectives: IUPHAR review 35.

机构信息

Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Melbourne, Victoria, Australia.

William Harvey Research Institute, Barts and the London School of Medicine, Queen Mary University of London, London, UK.

出版信息

Br J Pharmacol. 2022 Oct;179(19):4617-4639. doi: 10.1111/bph.15919. Epub 2022 Jul 29.

Abstract

We discuss the fascinating pharmacology of formylpeptide receptor 2 (FPR2; often referred to as FPR2/ALX since it binds lipoxin A ). Initially identified as a low-affinity 'relative' of FPR1, FPR2 presents complex and diverse biology. For instance, it is activated by several classes of agonists (from peptides to proteins and lipid mediators) and displays diverse expression patterns on myeloid cells as well as epithelial cells and endothelial cells, to name a few. Over the last decade, the pharmacology of FPR2 has progressed from being considered a weak chemotactic receptor to a master-regulator of the resolution of inflammation, the second phase of the acute inflammatory response. We propose that exploitation of the biology of FPR2 offers innovative ways to rectify chronic inflammatory states and represents a viable avenue to develop novel therapies. Recent elucidation of FPR2 structure will facilitate development of the anti-inflammatory and pro-resolving drugs of next decade.

摘要

我们探讨了受体内(formylpeptide receptor 2,FPR2;因其能结合脂氧素 A,通常也被称为 FPR2/ALX)激动剂的迷人药理学。FPR2 最初被鉴定为 FPR1 的低亲和力“相关受体”,具有复杂多样的生物学功能。例如,它可被几类激动剂(从肽到蛋白质和脂质介质)激活,并在髓样细胞以及上皮细胞和内皮细胞等多种细胞上呈现出不同的表达模式。在过去的十年中,FPR2 的药理学已从被认为是一种弱趋化性受体发展为炎症消退、急性炎症反应第二阶段的主要调控者。我们提出,利用 FPR2 的生物学特性为纠正慢性炎症状态提供了创新的方法,并为开发新的治疗方法提供了可行的途径。最近对 FPR2 结构的阐明将有助于开发下一个十年的抗炎和促解决药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/56ae/9545948/1c6a63af6f91/BPH-179-4617-g002.jpg

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