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GPR87

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Target not currently curated in GtoImmuPdb

Target id: 122

Nomenclature: GPR87

Family: Class A Orphans

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 7 358 3q25.1 GPR87 G protein-coupled receptor 87 4
Mouse 7 358 3 D Gpr87 G protein-coupled receptor 87
Rat 7 358 2q31 Gpr87 G protein-coupled receptor 87
Previous and Unofficial Names Click here for help
FKSG78 | GPR95
Database Links Click here for help
Specialist databases
GPCRdb gpr87_human (Hs), gpr87_mouse (Mm)
Other databases
Alphafold Q9BY21 (Hs), Q99MT7 (Mm)
ChEMBL Target CHEMBL4523915 (Hs)
Ensembl Gene ENSG00000138271 (Hs), ENSMUSG00000051431 (Mm), ENSRNOG00000013894 (Rn)
Entrez Gene 53836 (Hs), 84111 (Mm), 310443 (Rn)
Human Protein Atlas ENSG00000138271 (Hs)
KEGG Gene hsa:53836 (Hs), mmu:84111 (Mm), rno:310443 (Rn)
OMIM 606379 (Hs)
Pharos Q9BY21 (Hs)
RefSeq Nucleotide NM_023915 (Hs), NM_032399 (Mm), NM_001107677 (Rn)
RefSeq Protein NP_076404 (Hs), NP_115775 (Mm), NP_001101147 (Rn)
UniProtKB Q9BY21 (Hs), Q99MT7 (Mm)
Wikipedia GPR87 (Hs)
Natural/Endogenous Ligands Click here for help
LPA
Comments: Proposed ligand, single publication

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Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
LPA Small molecule or natural product Click here for species-specific activity table Ligand is endogenous in the given species Hs Agonist 7.4 pEC50 2-3
⤷ pEC50 7.4 [2-3]
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
Ki16425 Small molecule or natural product Click here for species-specific activity table Hs Antagonist - - 3
⤷ [3]
dioctanoylglycerol pyrophosphate Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Antagonist - - 3
⤷ [3]
Antagonist Comments
The LPA-induced [Ca2+]i increase is blocked by the LPA receptor antagonist, Ki16425 and DGPP suggesting that these may be antagonists [3].
Tissue Distribution Click here for help
Squamous cell carcinomas
Expression level:  High
Species:  Human
Technique:  Transcription profiling, siRNA analyses, Immunoblotting, Immunohistochemistry
References:  1
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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Biologically Significant Variants Click here for help
Type:  Single nucleotide polymorphism
Species:  Human
Amino acid change:  T205M
Global MAF (%):  <1
Subpopulation MAF (%):  AFR: 1
Minor allele count:  A=0.002/4
Comment on frequency:  Low frequency (<10% in all tested populations)
SNP accession:  VAR_055921, rs35521104
Validation:  1000 Genomes, Frequency, Multiple observations
Type:  Naturally occurring SNP
Species:  Human
Amino acid change:  V260G
SNP accession:  rs76418398
Type:  Naturally occurring SNP
Species:  Human
Amino acid change:  S244X
Comment on frequency:  Low frequency (<10% of all tested populations)
SNP accession:  rs79475431
Type:  Naturally occurring SNP
Species:  Human
Amino acid change:  V171G
Comment on frequency:  Low frequency (<10% of all tested populations)
SNP accession:  rs79977940

References

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1. Glatt S, Halbauer D, Heindl S, Wernitznig A, Kozina D, Su KC, Puri C, Garin-Chesa P, Sommergruber W. (2008) hGPR87 contributes to viability of human tumor cells. Int J Cancer, 122 (9): 2008-16. [PMID:18183596]

2. Murakami M, Shiraishi A, Tabata K, Fujita N. (2008) Identification of the orphan GPCR, P2Y(10) receptor as the sphingosine-1-phosphate and lysophosphatidic acid receptor. Biochem Biophys Res Commun, 371 (4): 707-12. [PMID:18466763]

3. Tabata K, Baba K, Shiraishi A, Ito M, Fujita N. (2007) The orphan GPCR GPR87 was deorphanized and shown to be a lysophosphatidic acid receptor. Biochem Biophys Res Commun, 363 (3): 861-6. [PMID:17905198]

4. Wittenberger T, Schaller HC, Hellebrand S. (2001) An expressed sequence tag (EST) data mining strategy succeeding in the discovery of new G-protein coupled receptors. J Mol Biol, 307 (3): 799-813. [PMID:11273702]

Contributors

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