GPR139

GPR139
Identifiers
Aliases	GPR139, GPRg1, PGR3, G protein-coupled receptor 139
External IDs	OMIM: 618448; MGI: 2685341; HomoloGene: 45860; GeneCards: GPR139; OMA:GPR139 - orthologs
Gene location (Human)
Chr.	Chromosome 16 (human)
End	20,073,890 bp
Gene location (Mouse)
Chr.	Chromosome 7 (mouse)
End	118,783,826 bp
RNA expression pattern
	Top expressed in
	testicle; ; caudate nucleus; ; putamen; ; nucleus accumbens; ; hypothalamus; ; bone marrow; ; substantia nigra; ; pituitary gland; ; C1 segment; ; muscle tissue;
	Top expressed in
	lumbar spinal ganglion; ; habenula; ; medial vestibular nucleus; ; deep cerebellar nuclei; ; mammillary body; ; dorsal tegmental nucleus; ; dorsomedial hypothalamic nucleus; ; lateral hypothalamus; ; central gray substance of midbrain; ; embryo;
	More reference expression data
	; ;
	More reference expression data
Gene ontology
Molecular function	G protein-coupled receptor activity; protein dimerization activity; signal transducer activity; neuropeptide receptor activity;
Cellular component	integral component of membrane; plasma membrane; membrane;
Biological process	G protein-coupled receptor signaling pathway; phospholipase C-activating G protein-coupled receptor signaling pathway; neuropeptide signaling pathway; signal transduction;
	Sources:Amigo / QuickGO
Orthologs
	124274
	209776
	ENSG00000180269
	ENSMUSG00000066197
	Q6DWJ6
	Q80UC8
	NM_001002911; NM_001318483
	NM_001024138
	NP_001002911; NP_001305412
	NP_001019309
	Wikidata
View/Edit Human	View/Edit Mouse

G-protein coupled receptor 139 (GPC139) is a protein that in humans is encoded by the GPR139 gene.^[5]^[6] Recent research ('21) has shown that mice with loss of GCP139 experience schizophrenia-like symptomatology that is rescued with the dopamine receptor antagonist haloperidol and the μ-opioid receptor antagonist naltrexone;^[7] as well, the recently developed, potent, and GPR139 receptor selective agonist TAK-041 (aka NBI-1065846)^[8] is currently undergoing trials to gauge the efficacy for treating psychiatric conditions such as major depressive disorder and the negative symptoms of schizophrenia.

References

^ ^a ^b ^c GRCh38: Ensembl release 89: ENSG00000180269 – Ensembl, May 2017
^ ^a ^b ^c GRCm38: Ensembl release 89: ENSMUSG00000066197 – Ensembl, May 2017
^ "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
^ "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.
^ Vassilatis DK, Hohmann JG, Zeng H, Li F, Ranchalis JE, Mortrud MT, et al. (April 2003). "The G protein-coupled receptor repertoires of human and mouse". Proceedings of the National Academy of Sciences of the United States of America. 100 (8): 4903–4908. Bibcode:2003PNAS..100.4903V. doi:10.1073/pnas.0230374100. PMC 153653. PMID 12679517.
^ "Entrez Gene: GPR139 G protein-coupled receptor 139".
^ Dao M, Stoveken HM, Cao Y, Martemyanov KA (March 2022). "The role of orphan receptor GPR139 in neuropsychiatric behavior". Neuropsychopharmacology. 47 (4): 902–913. doi:10.1038/s41386-021-00962-2. PMC 8882194. PMID 33479510. S2CID 231668867.
^ Reichard HA, Schiffer HH, Monenschein H, Atienza JM, Corbett G, Skaggs AW, et al. (August 2021). "Discovery of TAK-041: a Potent and Selective GPR139 Agonist Explored for the Treatment of Negative Symptoms Associated with Schizophrenia". Journal of Medicinal Chemistry. 64 (15): 11527–11542. doi:10.1021/acs.jmedchem.1c00820. PMID 34260228. S2CID 235908256.

Vanti WB, Nguyen T, Cheng R, Lynch KR, George SR, O'Dowd BF (May 2003). "Novel human G-protein-coupled receptors". Biochemical and Biophysical Research Communications. 305 (1): 67–71. doi:10.1016/S0006-291X(03)00709-5. PMID 12732197.
Ottolenghi C, Fellous M, Barbieri M, McElreavey K (March 2002). "Novel paralogy relations among human chromosomes support a link between the phylogeny of doublesex-related genes and the evolution of sex determination". Genomics. 79 (3): 333–343. doi:10.1006/geno.2002.6711. PMID 11863363.
Takeda S, Kadowaki S, Haga T, Takaesu H, Mitaku S (June 2002). "Identification of G protein-coupled receptor genes from the human genome sequence". FEBS Letters. 520 (1–3): 97–101. doi:10.1016/S0014-5793(02)02775-8. PMID 12044878. S2CID 7116392.
Gloriam DE, Schiöth HB, Fredriksson R (April 2005). "Nine new human Rhodopsin family G-protein coupled receptors: identification, sequence characterisation and evolutionary relationship". Biochimica et Biophysica Acta (BBA) - General Subjects. 1722 (3): 235–246. doi:10.1016/j.bbagen.2004.12.001. PMID 15777626.
Matsuo A, Matsumoto S, Nagano M, Masumoto KH, Takasaki J, Matsumoto M, et al. (May 2005). "Molecular cloning and characterization of a novel Gq-coupled orphan receptor GPRg1 exclusively expressed in the central nervous system". Biochemical and Biophysical Research Communications. 331 (1): 363–369. doi:10.1016/j.bbrc.2005.03.174. PMID 15845401.

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[refGRCh38Ensembl-1] GRCh38: Ensembl release 89: ENSG00000180269 – Ensembl, May 2017

[refGRCm38Ensembl-2] GRCm38: Ensembl release 89: ENSMUSG00000066197 – Ensembl, May 2017

[3] "Human PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.

[4] "Mouse PubMed Reference:". National Center for Biotechnology Information, U.S. National Library of Medicine.

[pmid12679517-5] Vassilatis DK, Hohmann JG, Zeng H, Li F, Ranchalis JE, Mortrud MT, et al. (April 2003). "The G protein-coupled receptor repertoires of human and mouse". Proceedings of the National Academy of Sciences of the United States of America. 100 (8): 4903–4908. Bibcode:2003PNAS..100.4903V. doi:10.1073/pnas.0230374100. PMC 153653. PMID 12679517.

[entrez-6] "Entrez Gene: GPR139 G protein-coupled receptor 139".

[7] Dao M, Stoveken HM, Cao Y, Martemyanov KA (March 2022). "The role of orphan receptor GPR139 in neuropsychiatric behavior". Neuropsychopharmacology. 47 (4): 902–913. doi:10.1038/s41386-021-00962-2. PMC 8882194. PMID 33479510. S2CID 231668867.

[8] Reichard HA, Schiffer HH, Monenschein H, Atienza JM, Corbett G, Skaggs AW, et al. (August 2021). "Discovery of TAK-041: a Potent and Selective GPR139 Agonist Explored for the Treatment of Negative Symptoms Associated with Schizophrenia". Journal of Medicinal Chemistry. 64 (15): 11527–11542. doi:10.1021/acs.jmedchem.1c00820. PMID 34260228. S2CID 235908256.

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References

Further reading