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] Research 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]^[8]

Ligands

Agonists

Zelatriazin (TAK-41), (NBI-1065846) a potent, and GPR139 receptor selective agonist ^[9] which was in clinical trials to gauge the efficacy for treating psychiatric conditions such as major depressive disorder and the negative symptoms of schizophrenia, but was later dropped from development.

Antagonists

JNJ-3792165

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.
^ Vedel L, Nøhr AC, Gloriam DE, Bräuner-Osborne H. Pharmacology and function of the orphan GPR139 G protein-coupled receptor. Basic Clin Pharmacol Toxicol. 2020 Jun;126 Suppl 6(Suppl 6):35-46. doi:10.1111/bcpt.13263 PMID 31132229
^ 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] Vedel L, Nøhr AC, Gloriam DE, Bräuner-Osborne H. Pharmacology and function of the orphan GPR139 G protein-coupled receptor. Basic Clin Pharmacol Toxicol. 2020 Jun;126 Suppl 6(Suppl 6):35-46. doi:10.1111/bcpt.13263 PMID 31132229

[9] 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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GPR139

Ligands

References

Further reading