<i>GPR61</i> | Class A Orphans | IUPHAR/BPS Guide to PHARMACOLOGY

GPR61

Target id: 110

Nomenclature: GPR61

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 GPR61 in GtoImmuPdb

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
GPCR3 | BALGR | biogenic amine receptor-like GPCR
Database Links
Specialist databases
GPCRDB gpr61_human (Hs), gpr61_mouse (Mm)
Other databases
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
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

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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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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
Type:  Naturally occurring SNP
Species:  Human
Amino acid change:  L218P
Comment on frequency:  Low frequency (<10% in all tested populations)
SNP accession: 
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].

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]

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: GPR61. Last modified on 16/06/2015. Accessed on 18/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=110.