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

GPR87

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

   GtoImmuPdb view: OFF :     Currently no data for GPR87 in GtoImmuPdb

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 Affinity Units 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 Affinity Units 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

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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
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

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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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How to cite this page

Anthony P. Davenport, Stephen Alexander, Joanna L. Sharman, Adam J. Pawson, Helen E. Benson, Amy E. Monaghan, Wen Chiy Liew, Chido Mpamhanga, Jim Battey, Richard V. Benya, Robert T. Jensen, Sadashiva Karnik, Evi Kostenis, Eliot Spindel, Laura Storjohann, Kalyan Tirupula, Tom I. Bonner, Richard Neubig, Jean-Philippe Pin, Michael Spedding, Anthony Harmar.
Class A Orphans: GPR87. Last modified on 16/06/2015. Accessed on 14/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=122.