Review Article

Anti-inflammatory signaling through G protein-coupled receptors

Yun-jun Ge1,2, Qi-wen Liao2, Ye-chun Xu3,4, Qiang Zhao4,5, Bei-li Wu3,4, Richard D. Ye1,2
1 Institute of Chinese Medical Sciences, University of Macau, Macau SAR, China
2 School of Life and Health Sciences, The Chinese University of Hong Kong, Shenzhen 518172, China
3 CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
4 University of Chinese Academy of Sciences, Beijing 100049, China
5 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
Correspondence to: Richard D. Ye: richardye@cuhk.edu.cn,
DOI: 10.1038/s41401-020-00523-1
Received: 1 June 2020
Accepted: 24 August 2020
Advance online: 15 October 2020

Abstract

G protein-coupled receptors (GPCRs) play important roles in human physiology. GPCRs are involved in immunoregulation including regulation of the inflammatory response. Chemotaxis of phagocytes and lymphocytes is mediated to a great extent by the GPCRs for chemoattractants including myriads of chemokines. Accumulation and activation of phagocytes at the site of inflammation contribute to local inflammatory response. A handful of GPCRs have been found to transduce anti-inflammatory signals that promote resolution of inflammation. These GPCRs interact with selected metabolites of arachdonic acid, such as lipoxins, and of omega-3 essential fatty acids, such as resolvins and protectins. Despite mounting evidence for the in vivo functions of these anti- inflammatory and pro-resolving ligands paired with their respective GPCRs, the underlying signaling mechanisms have not been fully delineated. The present review summarizes what we have learned about these GPCRs, their structures and signaling pathways
and the prospect of targeting these receptors for novel anti-inflammatory therapies.
Keywords: GPCRs inflammation chemotaxis specialized pro-resolving mediators lipoxins FPR2 ligand-biased signalin

Article Options

Download Citation

Cited times in Scopus