GPR84 is an orphan G protein-coupled receptor that is activated by medium-chain fatty acids and hydroxy fatty acids although these may not be its endogenous agonist.1 It is highly expressed on immune cells and expression levels rise after exposure to inflammatory stimuli.2 Potent synthetic agonists enhance proinflammatory signaling and macrophage effector functions.1 PSB-1584 is a potent synthetic exogenous agonist at GPR84, EC50=5 nM which is selective against other free fatty acid receptors and is metabolically stable when incubated with human liver microsomes.3 An important new tool for studying the physiology of GPR84.4
Luscombe et al. (2020), 20 Years an Orphan: Is GPR84 a Plausible Medium-Chain Fatty Acid-Sensing Receptor?; DNA Cell Biol., 39 1926
Marsango et al (2020) Therapeutic validation of an orphan G protein-coupled receptor: The case of GPR84. Br. J. Pharmacol. Sept 1 (Online Ahead of Print)
Pilaiyar et al. (2018), 6-(Ar)Alkylamino-substituted Uracil Derivatives: Lipid Mimetics with Potent Activity at the Orphan G Protein-Coupled Receptor 84 (GPR84); ACS Omega, 3 3365
Chen et al. (2020), Modulation of the G-Protein-Coupled Receptor 84 (GPR84) by Agonists and Antagonists; J. Med. Chem. 63 15399
