GPR42, GPR84 | G protein-coupled receptors | IUPHAR/BPS Guide to PHARMACOLOGY

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GPR42, GPR84 C

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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There is some evidence to suggest that GPR42 and GPR84 may be free fatty acid receptors.

Receptors

GPR42 C Show summary »« Hide summary More detailed page go icon to follow link

Target Id	228
Nomenclature	GPR42
Previous and unofficial names	FFAR1L \| GPR41L \| FFAR3L \| G protein-coupled receptor 42 (gene/pseudogene)
Genes	GPR42 (Hs)
Ensembl ID	ENSG00000126251 (Hs)
UniProtKB AC	O15529 (Hs)
Principal transduction	-

GPR84 C Show summary »« Hide summary More detailed page go icon to follow link

Target Id

120

Nomenclature

GPR84

Previous and unofficial names

GPCR4 | Inflammation-related G-protein coupled receptor EX33

Genes

GPR84 (Hs), Gpr84 (Mm), Gpr84 (Rn)

Ensembl ID

ENSG00000139572 (Hs), ENSMUSG00000063234 (Mm), ENSRNOG00000036834 (Rn)

UniProtKB AC

Q9NQS5 (Hs), Q8CIM5 (Mm)

Principal transduction

G_i/G_o family

Agonists

DL-175 (orthosteric) [2,7]

decanoic acid [4,6]

undecanoic acid [6]

lauric acid [6]

Embelin (orthosteric) [2]

PSB-16434 (orthosteric) [2]

ZQ-16 (orthosteric) [2]

6-nonylpyridine-2,4-diol (orthosteric) [2]

Allosteric modulators

DIM (Agonist) [2]

Comment

Medium chain free fatty acids with carbon chain lengths of 9-14 activate GPR84 [5-6]. A surrogate ligand for GPR84, 6-n-octylaminouracil has also been proposed [5]. See review [1] for discussion of classification. Mutational analysis and molecular modelling of GPR84 has been reported [3].

References

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1. Davenport AP, Alexander SP, Sharman JL, Pawson AJ, Benson HE, Monaghan AE, Liew WC, Mpamhanga CP, Bonner TI, Neubig RR et al.. (2013) International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: recommendations for new pairings with cognate ligands. Pharmacol Rev, 65 (3): 967-86. [PMID:23686350]

2. Marsango S, Barki N, Jenkins L, Tobin AB, Milligan G. (2022) Therapeutic validation of an orphan G protein-coupled receptor: The case of GPR84. Br J Pharmacol, 179 (14): 3529-3541. [PMID:32869860]

3. Nikaido Y, Koyama Y, Yoshikawa Y, Furuya T, Takeda S. (2015) Mutation analysis and molecular modeling for the investigation of ligand-binding modes of GPR84. J Biochem, 157 (5): 311-20. [PMID:25425658]

4. Southern C, Cook JM, Neetoo-Isseljee Z, Taylor DL, Kettleborough CA, Merritt A, Bassoni DL, Raab WJ, Quinn E, Wehrman TS et al.. (2013) Screening β-Arrestin Recruitment for the Identification of Natural Ligands for Orphan G-Protein-Coupled Receptors. J Biomol Screen, 18 (5): 599-609. [PMID:23396314]

5. Suzuki M, Takaishi S, Nagasaki M, Onozawa Y, Iino I, Maeda H, Komai T, Oda T. (2013) Medium-chain Fatty Acid-sensing Receptor, GPR84, Is a Proinflammatory Receptor. J Biol Chem, 288 (15): 10684-91. [PMID:23449982]

6. Wang J, Wu X, Simonavicius N, Tian H, Ling L. (2006) Medium-chain fatty acids as ligands for orphan G protein-coupled receptor GPR84. J Biol Chem, 281 (45): 34457-64. [PMID:16966319]

7. Wang P, Raja A, Luscombe VB, Bataille CJR, Lucy D, Rogga VV, Greaves DR, Russell AJ. (2024) Development of Highly Potent, G-Protein Pathway Biased, Selective, and Orally Bioavailable GPR84 Agonists. J Med Chem, 67 (1): 110-137. [PMID:38146625]

How to cite this family page

Database page citation (select format):

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Christopoulos A, Davenport AP, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors. Br J Pharmacol. 180 Suppl 2:S23-S144.