20 years an orphan: is GPR84 a plausible medium-chain fatty acid-sensing receptor?

VB Luscombe, D Lucy, CJR Bataille… - DNA and Cell …, 2020 - liebertpub.com
GPR84 is an inflammation-induced receptor highly expressed on immune cells, yet its
endogenous ligand is still unknown. This makes any interpretation of its physiological …

Emerging opportunities to treat idiopathic pulmonary fibrosis: Design, discovery, and optimizations of small-molecule drugs targeting fibrogenic pathways

W Luo, Y Gu, S Fu, J Wang, J Zhang, Y Wang - European Journal of …, 2023 - Elsevier
Idiopathic pulmonary fibrosis (IPF) is the most common fibrotic form of idiopathic diffuse lung
disease. Due to limited treatment options, IPF patients suffer from poor survival. About ten …

[HTML][HTML] Structural insights into ligand recognition and activation of the medium-chain fatty acid-sensing receptor GPR84

H Liu, Q Zhang, X He, M Jiang, S Wang, X Yan… - nature …, 2023 - nature.com
GPR84 is an orphan class AG protein-coupled receptor (GPCR) that is predominantly
expressed in immune cells and plays important roles in inflammation, fibrosis, and …

[HTML][HTML] Free fatty acids signature in human intestinal disorders: Significant association between butyric acid and celiac disease

S Baldi, M Menicatti, G Nannini, E Niccolai, E Russo… - Nutrients, 2021 - mdpi.com
Altered circulating levels of free fatty acids (FFAs), namely short chain fatty acids (SCFAs),
medium chain fatty acids (MCFAs), and long chain fatty acids (LCFAs), are associated with …

A community biased signaling atlas

J Caroli, A Mamyrbekov, K Harpsøe, S Gardizi… - Nature Chemical …, 2023 - nature.com
Biased signaling gives hormones, probes or drugs distinct functional outcomes via the same
receptor. The Biased Signaling Atlas (https://BiasedSignalingAtlas. org) provides a …

[HTML][HTML] Medium-chain fatty acids suppress lipotoxicity-induced hepatic fibrosis via the immunomodulating receptor GPR84

R Ohue-Kitano, H Nonaka, A Nishida, Y Masujima… - JCI insight, 2023 - ncbi.nlm.nih.gov
Abstract Medium-chain triglycerides (MCTs), which consist of medium-chain fatty acids
(MCFAs), are unique forms of dietary fat with various health benefits. G protein–coupled 84 …

Phosphodiesters as GPR84 antagonists for the treatment of ulcerative colitis

LH Chen, Q Zhang, YF Xiao, YC Fang… - Journal of Medicinal …, 2022 - ACS Publications
GPR84 is a proinflammatory G protein-coupled receptor associated with several
inflammatory and fibrotic diseases. GPR84 antagonists have been evaluated in clinical trials …

Therapeutic validation of an orphan G protein‐coupled receptor: The case of GPR84

S Marsango, N Barki, L Jenkins… - British Journal of …, 2022 - Wiley Online Library
Despite the importance of members of the GPCR superfamily as targets of a broad range of
effective medicines many GPCRs remain poorly characterised. GPR84 is an example …

Modulation of the G-protein-coupled receptor 84 (GPR84) by agonists and antagonists

LH Chen, Q Zhang, X Xie, FJ Nan - Journal of Medicinal …, 2020 - ACS Publications
Since the discovery of medium-chain fatty acids as GPR84 ligands, significant
advancements have been made in the development of GPR84 agonists and antagonists …

[HTML][HTML] Overcoming resistance to immunotherapy by targeting GPR84 in myeloid-derived suppressor cells

G Qin, S Liu, J Liu, H Hu, L Yang, Q Zhao, C Li… - … and Targeted Therapy, 2023 - nature.com
Myeloid-derived suppressor cells (MDSCs) were found to gradually accumulate in the
orthotopic esophageal cancer mouse model during tumor progression. Although the roles of …