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oxoglutarate receptor

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Target id: 162

Nomenclature: oxoglutarate receptor

Family: Oxoglutarate receptor

This receptor has a proposed ligand; see the Latest Pairings page for more information.

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 337 13q32.1 OXGR1 oxoglutarate receptor 1
Mouse 7 337 14 E4 Oxgr1 oxoglutarate (alpha-ketoglutarate) receptor 1
Rat 7 337 15q24 Oxgr1 oxoglutarate receptor 1
Previous and Unofficial Names Click here for help
P2RY15 | GPR80 | GPR99 | P2Y15 | 2-oxoglutarate receptor 1 | Alpha-ketoglutarate receptor 1 | G protein-coupled receptor 99 | P2Y purinoceptor 15 | G protein-coupled receptor 80
Database Links Click here for help
Specialist databases
GPCRdb oxgr1_human (Hs), oxgr1_mouse (Mm), oxgr1_rat (Rn)
Other databases
Alphafold Q96P68 (Hs), Q6IYF8 (Mm), Q6Y1R5 (Rn)
ChEMBL Target CHEMBL2150840 (Hs), CHEMBL2325 (Rn)
Ensembl Gene ENSG00000165621 (Hs), ENSMUSG00000044819 (Mm), ENSRNOG00000037884 (Rn)
Entrez Gene 27199 (Hs), 239283 (Mm), 290493 (Rn)
Human Protein Atlas ENSG00000165621 (Hs)
KEGG Gene hsa:27199 (Hs), mmu:239283 (Mm), rno:290493 (Rn)
OMIM 606922 (Hs)
Pharos Q96P68 (Hs)
RefSeq Nucleotide NM_080818 (Hs), NM_001001490 (Mm), NM_207588 (Rn)
RefSeq Protein NP_543008 (Hs), NP_001001490 (Mm), NP_997471 (Rn)
UniProtKB Q96P68 (Hs), Q6IYF8 (Mm), Q6Y1R5 (Rn)
Wikipedia OXGR1 (Hs)
Natural/Endogenous Ligands Click here for help
α-ketoglutaric acid

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]LTE4 Small molecule or natural product Ligand is labelled Ligand is radioactive Mm Agonist 8.6 pKd 4
⤷ pKd 8.6 (Kd 2.5x10-9 M) [4]
α-ketoglutaric acid Small molecule or natural product Ligand is endogenous in the given species Ligand has a PDB structure Hs Full agonist 3.3 – 4.5 pEC50 2,7
⤷ pEC50 3.3 – 4.5 (EC50 6.9x10-5 – 3.2x10-5 M) [2,7]
View species-specific agonist tables
Agonist Comments
It was reported that OXGR1 responded to adenosine monophosphate (AMP) and adenosine [3]. However, this claim has been retracted [1].
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  2
Tissue Distribution Click here for help
Mast cells
Species:  Human
Technique:  Microarray analysis
References:  3
Kidney and placenta
Species:  Human
Technique:  Northern blot
References:  8
Trachea, salivary glands, kidney, fetal brain and lung showed the highest expression levels among the tissues examined.
Species:  Human
Technique:  RT-PCR
References:  3
Kidney, testis and smooth muscle
Species:  Mouse
Technique:  RT-PCR
References:  2
Distal tubules in the cortical region of kidney
Species:  Mouse
Technique:  in situ hybridisation
References:  2
Tissue Distribution Comments
No transcripts of OXGR1 were detected by Northern blot analysis in human brain tissues including the frontal cortex, caudate putamen, thalamus, hypothalamus, hippocampus and pons tissues [5].
Expression Datasets Click here for help

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Gene Expression and Pathophysiology Comments
DNA hypermethylation of OXGR1 is found to occur frequently in hepatocellular carcinoma [6]. It is also shown that restoration of the OXGR1 expression enhanced the sensitivity of hepatoma cell lines to anticancer drugs, 5-fluorouracil and doxorubicin [6].
Biologically Significant Variants Click here for help
Type:  Naturally occurring SNP
Species:  Human
Description:  R63G
SNP accession:  rs9300380

References

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1. Abbracchio MP, Burnstock G, Boeynaems JM, Barnard EA, Boyer JL, Kennedy C, Miras-Portugal MT, King BF, Gachet C, Jacobson KA et al.. (2005) The recently deorphanized GPR80 (GPR99) proposed to be the P2Y15 receptor is not a genuine P2Y receptor. Trends Pharmacol Sci, 26 (1): 8-9. [PMID:15629198]

2. He W, Miao FJ, Lin DC, Schwandner RT, Wang Z, Gao J, Chen JL, Tian H, Ling L. (2004) Citric acid cycle intermediates as ligands for orphan G-protein-coupled receptors. Nature, 429 (6988): 188-93. [PMID:15141213]

3. Inbe H, Watanabe S, Miyawaki M, Tanabe E, Encinas JA. (2004) Identification and characterization of a cell-surface receptor, P2Y15, for AMP and adenosine. J Biol Chem, 279 (19): 19790-9. [PMID:15001573]

4. Kanaoka Y, Maekawa A, Austen KF. (2013) Identification of GPR99 protein as a potential third cysteinyl leukotriene receptor with a preference for leukotriene E4 ligand. J Biol Chem, 288 (16): 10967-72. [PMID:23504326]

5. Lee DK, Nguyen T, Lynch KR, Cheng R, Vanti WB, Arkhitko O, Lewis T, Evans JF, George SR, O'Dowd BF. (2001) Discovery and mapping of ten novel G protein-coupled receptor genes. Gene, 275 (1): 83-91. [PMID:11574155]

6. Lu CY, Hsieh SY, Lu YJ, Wu CS, Chen LC, Lo SJ, Wu CT, Chou MY, Huang TH, Chang YS. (2009) Aberrant DNA methylation profile and frequent methylation of KLK10 and OXGR1 genes in hepatocellular carcinoma. Genes Chromosomes Cancer, 48 (12): 1057-68. [PMID:19760608]

7. 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]

8. Wittenberger T, Hellebrand S, Munck A, Kreienkamp HJ, Schaller HC, Hampe W. (2002) GPR99, a new G protein-coupled receptor with homology to a new subgroup of nucleotide receptors. BMC Genomics, 3: 17. [PMID:12098360]

Contributors

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