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

Abstract:

: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.

journal_name

Br J Pharmacol

authors

Marsango S,Barki N,Jenkins L,Tobin AB,Milligan G

doi

10.1111/bph.15248

subject

Has Abstract

pub_date

2020-09-01 00:00:00

eissn

0007-1188

issn

1476-5381

pub_type

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