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GPR61

Family: Class A Orphans

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Antagonists
Transduction Mechanisms
Tissue Distribution
Expression Datasets
Physiological Consequences of Altering Gene Expression
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 7 451 1p13.3 GPR61 G protein-coupled receptor 61 1
Mouse 7 449 3 F3 Gpr61 G protein-coupled receptor 61
Rat 7 449 2q34 Gpr61 G protein-coupled receptor 61
Previous and Unofficial Names
BALGR
GPCR3
GPR61
G protein-coupled receptor 61
Biogenic amine receptor-like G-protein coupled receptor
probable G-protein coupled receptor 61
biogenic amine receptor-like GPCR
Gpr61_predicted
LOC310780
G protein-coupled receptor 61 (predicted)
Database Links
Ensembl ENSG00000156097 (Hs), ENSMUSG00000046793 (Mm), ENSRNOG00000019738 (Rn)
Entrez Gene 83873 (Hs), 229714 (Mm), 310780 (Rn)
GeneCards GPR61 (Hs)
GenitoUrinary Development Molecular Anatomy Project Gpr61 (Mm)
HomoloGene 12910 (Hs)
Human Protein Reference Database 06077 (Hs)
InterPro Q9BZJ8 (Hs), Q8C010 (Mm)
KEGG Gene hsa:83873 (Hs), mmu:229714 (Mm), rno:310780 (Rn)
OMIM 606916 (Hs)
PharmGKB Gene PA28905 (Hs)
Protein Ontology (PRO) PRO:000001535 (Hs)
RefSeq Nucleotide NM_031936 (Hs), NM_175470 (Mm), NM_001107715 (Rn)
RefSeq Protein NP_114142 (Hs), NP_780679 (Mm), NP_001101185 (Rn)
TreeFam ENSG00000156097 (Hs), ENSMUSG00000046793 (Mm), ENSRNOG00000019738 (Rn)
UniGene Hs. 514690 (Hs)
UniProt Q9BZJ8 (Hs), Q8C010 (Mm)
Wikipedia GPR61
Orphan and other 7TM receptors
Antagonist Comments
Although no endogenous ligands have been identified, 5-(nonyloxy)tryptamine has been reported to be a low affinity inverse agonist [3].
Primary Transduction Mechanisms
Comments:  The receptor displays constitutive activity that is abolished by deletion of the N-terminal 25 amino acids [4].
References:  4
Tissue Distribution
Brain, testes
Species:  Human
Technique:  Semi-quantitative PCR
References:  1
Cerebral cortex, occipital pole, frontal lobe, temporal lobe, amygdala, hippocampus (lower expression in putamen and caudate nucleus)
Species:  Human
Technique:  Northern blot
References:  1
Dentate gyrus, hippocampus, cerebral cortex (moderate to weak expression in hypothalamus, central amygdala, nucleus accumbens and nucleus tractus solitarius)
Species:  Mouse
Technique:  RT-PCR
References:  2
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 Consequences of Altering Gene Expression
GPR61 deficient mice exhibit obesity associated with hyperphagia. Significantly lower mRNA levels of pro-opiomelanocortin and brain-derived neurotropic factor mRNAs in hypothalamus compared to wild type. Phenotype displayed: hyperphagia, increased visceral fat pad weight, increased liver weight and triglyceride content, increased plasma leptin and insulin levels.
Species:  Mouse
Tissue:  Live, adipose, plasma
Technique:  Targeted gene disruption
References:  2
Gene Expression and Pathophysiology Comments
Mouse models of GPR61 disruption indicate a role for the receptor in regulation of appetite and body weight, indicating that the receptor may be a therapeutic target for obesity and eating disorders.
Biologically Significant Variants
L218P, low frequency (<10% in all tested populations)
SNP accession:  rs75311269 
Type:  Naturally occurring SNPs.
Species:  Human
References: 
General Comments
Site-directed mutagenesis studies suggest a possible role for the N-terminal 25 amino acids of the receptor in constitutive activity and for membrane translocation of the receptor [4].
Available Assays
DiscoveRx PathHunter® CHO-K1 GPR61 (Orphan) High Expression β-Arrestin Cell Line Human Cat No. 93-0407C2A
DiscoveRx PathHunter® eXpress GPR61 CHO-K1 β-Arrestin (Orphan) GPCR Assay Human Cat No. 93-0407E2ACP1

REFERENCES

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1. Cikos, S; Gregor, P; Koppel, J. (2001) Cloning of a novel biogenic amine receptor-like G protein-coupled receptor expressed in human brain. Biochim. Biophys. Acta, 1521 (1-3): 66-72. [PMID:11690637]

2. Nambu, H; Fukushima, M; Hikichi, H; Inoue, T; Nagano, N; Tahara, Y; Nambu, T; Ito, J; Ogawa, Y; Ozaki, S; et al.. (2011) Characterization of metabolic phenotypes of mice lacking GPR61, an orphan G-protein coupled receptor. Life Sci., 89 (21-22): 765-72. [PMID:21971119]

3. Takeda, S; Okada, T; Okamura, M; Haga, T; Isoyama-Tanaka, J; Kuwahara, H; Minamino, N. (2004) The receptor-Galpha fusion protein as a tool for ligand screening: a model study using a nociceptin receptor-Galphai2 fusion protein. J. Biochem., 135 (5): 597-604. [PMID:15173198]

4. Toyooka, M; Tujii, T; Takeda, S. (2009) The N-terminal domain of GPR61, an orphan G-protein-coupled receptor, is essential for its constitutive activity. J. Neurosci. Res., 87 (6): 1329-33. [PMID:19025769]

To cite this database page, please use the following:

Amy E. Monaghan.
Class A Orphans: GPR61. Last modified on 02/11/2012. Accessed on 26/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=110.


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