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GPR63

Family: Class A Orphans

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Agonists
Tissue Distribution
Expression Datasets
Physiological Functions
Gene Expression and Pathophysiology
Biologically Significant Variants
General Comments
References
Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 419 6q16.1-q16.3 GPR63 G protein-coupled receptor 63 3-5
Mouse 7 425 4 A3 Gpr63 G protein-coupled receptor 63 3
Rat 7 425 5q21 Gpr63 G protein-coupled receptor 63
Previous and Unofficial Names
PSP24B
PSP24(beta)
PSP24-2
Gpr63_predicted
LOC297952
G protein-coupled receptor 63
G protein-coupled receptor 63 (predicted)
probable G-protein coupled receptor 63
PSP24beta
Database Links
Ensembl ENSG00000112218 (Hs), ENSMUSG00000040372 (Mm), ENSRNOG00000007675 (Rn)
Entrez Gene 81491 (Hs), 81006 (Mm), 297952 (Rn)
GeneCards GPR63 (Hs)
GenitoUrinary Development Molecular Anatomy Project Gpr63 (Mm)
HomoloGene 12759 (Hs)
Human Protein Reference Database 06076 (Hs)
InterPro Q9BZJ6 (Hs), Q9EQQ3 (Mm)
KEGG Gene hsa:81491 (Hs), mmu:81006 (Mm), rno:297952 (Rn)
OMIM 606915 (Hs)
PharmGKB Gene PA28907 (Hs)
Protein Ontology (PRO) PRO:000001647 (Hs)
RefSeq Nucleotide NM_030784 (Hs), NM_030733 (Mm), NM_001106640 (Rn)
RefSeq Protein NP_110411 (Hs), NP_109658 (Mm), NP_001100110 (Rn)
TreeFam ENSG00000112218 (Hs), ENSMUSG00000040372 (Mm), ENSRNOG00000007675 (Rn)
UniGene Hs. 632612 (Hs)
UniProt Q9BZJ6 (Hs), Q9EQQ3 (Mm)
Wikipedia GPR63
Orphan and other 7TM receptors
Natural/Endogenous Ligand(s)
Comments: Proposed ligand, single publication
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
dioleoyl phosphatidic acid Hs Full agonist 6.3 pEC50 5
dihydrosp​hingosine​-1-phosph​ate Hs Full agonist 6.17 pEC50 5
sphingosine 1-phosphate Hs Full agonist 6.1 – 6.18 pEC50 5
Agonist Comments
Yin et al. evaluated lipid receptor and ligand pairing using a β-arrestin assay system but there was no hit detected for GPR63 [6].
Tissue Distribution
Frontal cortex, thalamus, caudate, hypothalamus, midbrain
Species:  Human
Technique:  Northern blot
References:  4
High expression in brain, especially in the thalamus and the nucleus caudatus, and peripheral tissues such as thymus, stomach and small intestine. Lower expression in kidney, spleen, pancreases and heart.
Species:  Human
Technique:  RT-PCR
References:  5
Brain, neuroendocrine cells, testicular cells
Species:  Mouse
Technique:  Northern blot
References:  3
Neuronal cell
Species:  Rat
Technique:  Northern blot
References:  3
Tissue Distribution Comments
Expression of GPR63 was not detected in the liver when examined by Northern blot analysis [4].
Expression Datasets

Click here to show/hide data

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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Physiological Functions Comments
GPR63 is highly expressed in neuronal cells and the expression remains constant from the early embryonic stages to adulthood, suggesting the important roles of GPR63 in neuronal functions [3]. High expression of GPR63 in thalamus, caudate, stomach and small intestine may imply a role of GPR63 in central or peripheral control of feeding behavior [5].
Gene Expression and Pathophysiology Comments
A 1.5Mb deletion in chromosome 6q16.1, including GPR63, is associated with autistic features including speech delay [1].
Biologically Significant Variants
V21M, low frequency (<10% of all tested populations)
SNP accession:  rs35358396 
Type:  Naturally occurring SNPs.
Species:  Human
References: 
General Comments
Proposed ligands (sphingosine 1-phosphate and dioleoylphosphatidic acid), supported by one publication [5]. Unlike Xenopus GPR63, mammalian GPR63 is not responsive to lysophosphatidic acid (LPA) [2].

REFERENCES

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1. Derwińska, K; Bernaciak, J; Wiśniowiecka-Kowalnik, B; Obersztyn, E; Bocian, E; Stankiewicz, P. (2009) Autistic features with speech delay in a girl with an approximately 1.5-Mb deletion in 6q16.1, including GPR63 and FUT9. Clin. Genet., 75 (2): 199-202. [PMID:18717687]

2. Kawasawa, Y; Kume, K; Izumi, T; Shimizu, T. (2000) Mammalian PSP24s (alpha and beta isoforms) are not responsive to lysophosphatidic acid in mammalian expression systems. Biochem. Biophys. Res. Commun., 276 (3): 957-64. [PMID:11027575]

3. Kawasawa, Y; Kume, K; Nakade, S; Haga, H; Izumi, T; Shimizu, T. (2000) Brain-specific expression of novel G-protein-coupled receptors, with homologies to Xenopus PSP24 and human GPR45. Biochem. Biophys. Res. Commun., 276 (3): 952-6. [PMID:11027574]

4. Lee, DK; George, SR; Cheng, R; Nguyen, T; Liu, Y; Brown, M; Lynch, KR; O'Dowd, BF. (2001) Identification of four novel human G protein-coupled receptors expressed in the brain. Brain Res. Mol. Brain Res., 86 (1-2): 13-22. [PMID:11165367]

5. Niedernberg, A., Tunaru, S., Blaukat, A., Ardati, A. and Kostenis, E. (2003) Sphingosine 1-phosphate and dioleoylphosphatidic acid are low affinity agonists for the orphan receptor GPR63. Cell Signal, 15: 435-446. [PMID:12618218]

6. Yin, H., Chu, A., Li, W., Wang, B., Shelton, F., Otero, F., Nguyen, D.G., Caldwell, J.S. and Chen, Y.A. (2009) Lipid G protein-coupled receptor ligand identification using beta-arrestin PathHunter assay. J Biol Chem, 284: 12328-12338. [PMID:19286662]

To cite this database page, please use the following:

Wen Chiy Liew.
Class A Orphans: GPR63. Last modified on 02/11/2012. Accessed on 26/05/2013. IUPHAR database (IUPHAR-DB), http://iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=112.


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