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

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. Expression of GPR84 is strongly up regulated in immune cells in a range of pro‐inflammatory settings and clinical trials to treat...

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Published in:British journal of pharmacology 2022-07, Vol.179 (14), p.3529-3541
Main Authors: Marsango, Sara, Barki, Natasja, Jenkins, Laura, Tobin, Andrew B., Milligan, Graeme
Format: Article
Language:English
Subjects:
allosteric ligand
Antagonists
Clinical trials
Commissioned Review ‐ Themed Issue
Energy metabolism
Fibrosis
G protein-coupled receptors
GPCR
GPR84
Inflammation
Lung diseases
Membrane proteins
orphan receptor
orthosteric ligand
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Summary: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. Expression of GPR84 is strongly up regulated in immune cells in a range of pro‐inflammatory settings and clinical trials to treat idiopathic pulmonary fibrosis are currently ongoing using ligands with differing levels of selectivity and affinity as GPR84 antagonists. Although blockade of GPR84 may potentially prove effective also in diseases associated with inflammation of the lower gut there is emerging interest in defining if agonists of GPR84 might find utility in conditions in which regulation of metabolism or energy sensing is compromised. Here, we consider the physiological and pathological expression profile of GPR84 and, in the absence of direct structural information, recent developments and use of GPR84 pharmacological tool compounds to study its broader role and biology. LINKED ARTICLES This article is part of a themed issue on Structure Guided Pharmacology of Membrane Proteins (BJP 75th Anniversary). To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v179.14/issuetoc
ISSN:0007-1188
1476-5381
DOI:10.1111/bph.15248