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]

GPR139
Identifiers
AliasesGPR139, GPRg1, PGR3, G protein-coupled receptor 139
External IDsOMIM: 618448; MGI: 2685341; HomoloGene: 45860; GeneCards: GPR139; OMA:GPR139 - orthologs
Orthologs
SpeciesHumanMouse
Entrez
Ensembl
UniProt
RefSeq (mRNA)

NM_001002911
NM_001318483

NM_001024138

RefSeq (protein)

NP_001002911
NP_001305412

NP_001019309

Location (UCSC)Chr 16: 20.03 – 20.07 MbChr 7: 118.74 – 118.78 Mb
PubMed search[3][4]
Wikidata
View/Edit HumanView/Edit Mouse

Ligands

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Agonists


Antagonists

References

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  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000180269Ensembl, May 2017
  2. ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000066197Ensembl, 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.
  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 12679517.4903-4908&rft.date=2003-04&rft_id=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC153653#id-name=PMC&rft_id=info:pmid/12679517&rft_id=info:doi/10.1073/pnas.0230374100&rft_id=info:bibcode/2003PNAS..100.4903V&rft.aulast=Vassilatis&rft.aufirst=DK&rft.au=Hohmann, JG&rft.au=Zeng, H&rft.au=Li, F&rft.au=Ranchalis, JE&rft.au=Mortrud, MT&rft.au=Brown, A&rft.au=Rodriguez, SS&rft.au=Weller, JR&rft.au=Wright, AC&rft.au=Bergmann, JE&rft.au=Gaitanaris, GA&rft_id=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC153653&rfr_id=info:sid/en.wikipedia.org:GPR139" class="Z3988">
  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 231668867.902-913&rft.date=2022-03&rft_id=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8882194#id-name=PMC&rft_id=https://api.semanticscholar.org/CorpusID:231668867#id-name=S2CID&rft_id=info:pmid/33479510&rft_id=info:doi/10.1038/s41386-021-00962-2&rft.aulast=Dao&rft.aufirst=M&rft.au=Stoveken, HM&rft.au=Cao, Y&rft.au=Martemyanov, KA&rft_id=https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8882194&rfr_id=info:sid/en.wikipedia.org:GPR139" class="Z3988">
  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 235908256.11527-11542&rft.date=2021-08&rft_id=https://api.semanticscholar.org/CorpusID:235908256#id-name=S2CID&rft_id=info:pmid/34260228&rft_id=info:doi/10.1021/acs.jmedchem.1c00820&rft.aulast=Reichard&rft.aufirst=HA&rft.au=Schiffer, HH&rft.au=Monenschein, H&rft.au=Atienza, JM&rft.au=Corbett, G&rft.au=Skaggs, AW&rft.au=Collia, DR&rft.au=Ray, WJ&rft.au=Serrats, J&rft.au=Bliesath, J&rft.au=Kaushal, N&rft.au=Lam, BP&rft.au=Amador-Arjona, A&rft.au=Rahbaek, L&rft.au=McConn, DJ&rft.au=Mulligan, VJ&rft.au=Brice, N&rft.au=Gaskin, PL&rft.au=Cilia, J&rft.au=Hitchcock, S&rfr_id=info:sid/en.wikipedia.org:GPR139" class="Z3988">

Further reading

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  • 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 12732197.67-71&rft.date=2003-05&rft_id=info:doi/10.1016/S0006-291X(03)00709-5&rft_id=info:pmid/12732197&rft.aulast=Vanti&rft.aufirst=WB&rft.au=Nguyen, T&rft.au=Cheng, R&rft.au=Lynch, KR&rft.au=George, SR&rft.au=O'Dowd, BF&rfr_id=info:sid/en.wikipedia.org:GPR139" class="Z3988">
  • 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 11863363.333-343&rft.date=2002-03&rft_id=info:doi/10.1006/geno.2002.6711&rft_id=info:pmid/11863363&rft.aulast=Ottolenghi&rft.aufirst=C&rft.au=Fellous, M&rft.au=Barbieri, M&rft.au=McElreavey, K&rfr_id=info:sid/en.wikipedia.org:GPR139" class="Z3988">
  • 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 7116392.1–3&rft.pages=97-101&rft.date=2002-06&rft_id=https://api.semanticscholar.org/CorpusID:7116392#id-name=S2CID&rft_id=info:pmid/12044878&rft_id=info:doi/10.1016/S0014-5793(02)02775-8&rft.aulast=Takeda&rft.aufirst=S&rft.au=Kadowaki, S&rft.au=Haga, T&rft.au=Takaesu, H&rft.au=Mitaku, S&rfr_id=info:sid/en.wikipedia.org:GPR139" class="Z3988">
  • 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 15777626.235-246&rft.date=2005-04&rft_id=info:doi/10.1016/j.bbagen.2004.12.001&rft_id=info:pmid/15777626&rft.aulast=Gloriam&rft.aufirst=DE&rft.au=Schiöth, HB&rft.au=Fredriksson, R&rfr_id=info:sid/en.wikipedia.org:GPR139" class="Z3988">
  • 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 15845401.363-369&rft.date=2005-05&rft_id=info:doi/10.1016/j.bbrc.2005.03.174&rft_id=info:pmid/15845401&rft.aulast=Matsuo&rft.aufirst=A&rft.au=Matsumoto, S&rft.au=Nagano, M&rft.au=Masumoto, KH&rft.au=Takasaki, J&rft.au=Matsumoto, M&rft.au=Kobori, M&rft.au=Katoh, M&rft.au=Shigeyoshi, Y&rfr_id=info:sid/en.wikipedia.org:GPR139" class="Z3988">