Members of the GPCR superfamily have a wide variety of physiological roles and are therefore valuable targets for developing effective medicines. However, within this superfamily are receptors that are less well characterized and remain orphans, including GPR84. This receptor is stimulated by ligands derived from dietary nutrients, specifically medium chain fatty acids (C9-14), and novel synthetic agonists. There are data demonstrating the role of GPR84 in inflammatory pathways, in addition to emerging data suggesting a key role for GPR84 as a nutrient-sensing GPCR involved in metabolism by sensing energy load via nutrient exposure and subsequent signalling leading to modulation of food intake. Exploring GPR84 pharmacology, its localization and what drives its expression has revealed multiple roles for this receptor. Here, we will reflect on these various roles of GRP84 demonstrated thus far, primarily by exploring data from pre-clinical and clinical studies in various physiological systems, with a specific focus on the gastrointestinal tract. LINKED ARTICLES: This article is part of a themed issue GPR84 Pharmacology. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v181.10/issuetoc.
Keywords: GPCR; GPR84; appetite; inflammation gastrointestinal tract (GIT); medium chain fatty acids (MCFAs); metabolism.
© 2023 The Authors. British Journal of Pharmacology published by John Wiley & Sons Ltd on behalf of British Pharmacological Society.