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{{Short description|Protein-coding gene in the species Homo sapiens}}
{{Short description|Protein-coding gene in the species Homo sapiens}}
{{Infobox_gene}}
{{Infobox_gene}}
'''G-protein coupled receptor 139''' (GPC139) is a [[protein]] that in humans is encoded by the ''GPR139'' [[gene]].<ref name="pmid12679517">{{cite journal | vauthors = Vassilatis DK, Hohmann JG, Zeng H, Li F, Ranchalis JE, Mortrud MT, Brown A, Rodriguez SS, Weller JR, Wright AC, Bergmann JE, Gaitanaris GA | display-authors = 6 | title = The G protein-coupled receptor repertoires of human and mouse | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 100 | issue = 8 | pages = 4903–4908 | date = April 2003 | pmid = 12679517 | pmc = 153653 | doi = 10.1073/pnas.0230374100 | doi-access = free | bibcode = 2003PNAS..100.4903V }}</ref><ref name="entrez">{{cite web | title = Entrez Gene: GPR139 G protein-coupled receptor 139| url = https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=124274}}</ref> 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]];<ref>{{cite journal | vauthors = Dao M, Stoveken HM, Cao Y, Martemyanov KA | title = The role of orphan receptor GPR139 in neuropsychiatric behavior | journal = Neuropsychopharmacology | volume = 47 | issue = 4 | pages = 902–913 | date = March 2022 | pmid = 33479510 | doi = 10.1038/s41386-021-00962-2 | pmc = 8882194 | s2cid = 231668867 }}</ref> as well, the recently developed, potent, and GPR139 receptor selective agonist TAK-041 (aka NBI-1065846)<ref>{{cite journal | vauthors = Reichard HA, Schiffer HH, Monenschein H, Atienza JM, Corbett G, Skaggs AW, Collia DR, Ray WJ, Serrats J, Bliesath J, Kaushal N, Lam BP, Amador-Arjona A, Rahbaek L, McConn DJ, Mulligan VJ, Brice N, Gaskin PL, Cilia J, Hitchcock S | display-authors = 6 | title = Discovery of TAK-041: a Potent and Selective GPR139 Agonist Explored for the Treatment of Negative Symptoms Associated with Schizophrenia | journal = Journal of Medicinal Chemistry | volume = 64 | issue = 15 | pages = 11527–11542 | date = August 2021 | pmid = 34260228 | doi = 10.1021/acs.jmedchem.1c00820 | s2cid = 235908256 }}</ref> is currently undergoing trials to gauge the efficacy for treating psychiatric conditions such as [[major depressive disorder]] and the negative symptoms of [[schizophrenia]].
'''G-protein coupled receptor 139''' (GPC139) is a [[protein]] that in humans is encoded by the ''GPR139'' [[gene]].<ref name="pmid12679517">{{cite journal | vauthors = Vassilatis DK, Hohmann JG, Zeng H, Li F, Ranchalis JE, Mortrud MT, Brown A, Rodriguez SS, Weller JR, Wright AC, Bergmann JE, Gaitanaris GA | display-authors = 6 | title = The G protein-coupled receptor repertoires of human and mouse | journal = Proceedings of the National Academy of Sciences of the United States of America | volume = 100 | issue = 8 | pages = 4903–4908 | date = April 2003 | pmid = 12679517 | pmc = 153653 | doi = 10.1073/pnas.0230374100 | doi-access = free | bibcode = 2003PNAS..100.4903V }}</ref><ref name="entrez">{{cite web | title = Entrez Gene: GPR139 G protein-coupled receptor 139| url = https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=124274}}</ref> 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]].<ref>{{cite journal | vauthors = Dao M, Stoveken HM, Cao Y, Martemyanov KA | title = The role of orphan receptor GPR139 in neuropsychiatric behavior | journal = Neuropsychopharmacology | volume = 47 | issue = 4 | pages = 902–913 | date = March 2022 | pmid = 33479510 | doi = 10.1038/s41386-021-00962-2 | pmc = 8882194 | s2cid = 231668867 }}</ref><ref>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}}</ref>
==Ligands==
;Agonists
* [[Zelatriazin|Zelatriazin (TAK-41)]], (NBI-1065846) a potent, and GPR139 receptor selective agonist <ref>{{cite journal | vauthors = Reichard HA, Schiffer HH, Monenschein H, Atienza JM, Corbett G, Skaggs AW, Collia DR, Ray WJ, Serrats J, Bliesath J, Kaushal N, Lam BP, Amador-Arjona A, Rahbaek L, McConn DJ, Mulligan VJ, Brice N, Gaskin PL, Cilia J, Hitchcock S | display-authors = 6 | title = Discovery of TAK-041: a Potent and Selective GPR139 Agonist Explored for the Treatment of Negative Symptoms Associated with Schizophrenia | journal = Journal of Medicinal Chemistry | volume = 64 | issue = 15 | pages = 11527–11542 | date = August 2021 | pmid = 34260228 | doi = 10.1021/acs.jmedchem.1c00820 | s2cid = 235908256 }}</ref> 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 ==
== References ==

Latest revision as of 08:11, 23 December 2023

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

124274

209776

Ensembl

ENSG00000180269

ENSMUSG00000066197

UniProt

Q6DWJ6

Q80UC8

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

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

[edit]
Agonists


Antagonists

References

[edit]
  1. ^ a b c GRCh38: Ensembl release 89: ENSG00000180269 – Ensembl, May 2017
  2. ^ a b c 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.
  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.
  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.

Further reading

[edit]
  • 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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