<i>GPR87</i> | Class A Orphans | IUPHAR/BPS Guide to PHARMACOLOGY

Top ▲

GPR87

Target not currently curated in GtoImmuPdb

Target id: 122

Nomenclature: GPR87

Family: Class A Orphans

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 358 3q24 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
FKSG78 | GPR95
Database Links
Specialist databases
GPCRDB gpr87_human (Hs), gpr87_mouse (Mm)
Other databases
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands
LPA
Comments: Proposed ligand, single publication

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 Value Parameter Reference
LPA 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 Hs Antagonist - - 3
[3]
dioctanoylglycerol pyrophosphate 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
Squamous cell carcinomas
Expression level:  High
Species:  Human
Technique:  Transcription profiling, siRNA analyses, Immunoblotting, Immunohistochemistry
References:  1
Expression Datasets

Show »

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]

There should be a chart of expression data here, you may need to enable JavaScript!
Biologically Significant Variants
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: 
Validation:  1000 Genomes, Frequency, Multiple observations
Type:  Naturally occurring SNP
Species:  Human
Amino acid change:  V260G
SNP accession: 
Type:  Naturally occurring SNP
Species:  Human
Amino acid change:  S244X
Comment on frequency:  Low frequency (<10% of all tested populations)
SNP accession: 
Type:  Naturally occurring SNP
Species:  Human
Amino acid change:  V171G
Comment on frequency:  Low frequency (<10% of all tested populations)
SNP accession: 

References

Show »

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

Show »

How to cite this page

Select citation format: