oxoglutarate receptor

Target id: 162

Nomenclature: oxoglutarate receptor

Family: Oxoglutarate receptor

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

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

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 337 13q32.2 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
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
Specialist databases
GPCRDB oxgr1_human (Hs), oxgr1_mouse (Mm), oxgr1_rat (Rn)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
InterPro
KEGG Gene
NeXtProt
OMIM
PharmGKB Gene
Protein Ontology (PRO)
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniProtKB
Wikipedia
Natural/Endogenous Ligands
α-ketoglutaric acid

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[3H]LTE4 Mm Agonist 8.6 pKd 4
pKd 8.6 (Kd 2.5x10-9 M) [4]
α-ketoglutaric acid 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 However, this claim has been retracted [1].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
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  2
Tissue Distribution
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
Mast cells
Species:  Human
Technique:  Microarray analysis
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

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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
Type:  Naturally occurring SNP
Species:  Human
Description:  R63G
SNP accession: 

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, Weisman GA. (2005) The recently deorphanized GPR80 (GPR99) proposed to be the P2Y15 receptor is not a genuine P2Y receptor. Trends Pharmacol Sci26: 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. Nature429: 188-193. [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 as a potential third cysteinyl leukotriene receptor with a preference for leukotriene E4. J. Biol. Chem.,  [Epub ahead of print]. [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. Gene275: 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 Cancer48 (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 Screen18 (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 Genomics3: 17. [PMID:12098360]

Contributors

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How to cite this page

Wen Chiy Liew.
Oxoglutarate receptor: oxoglutarate receptor. Last modified on 16/06/2015. Accessed on 25/02/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=162.