Login
Login

GPR139

{{cs1 config|name-list-style=vanc}}

{{Short description|Protein-coding gene in the species Homo sapiens}}

{{Infobox_gene}}

G-protein coupled receptor 139 (GPC139) is a protein that in humans is encoded by the GPR139 gene.{{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 }}{{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}} 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.{{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 }}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}}

Ligands

;Agonists

  • Zelatriazin (TAK-41), (NBI-1065846) a potent, and GPR139 receptor selective agonist {{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 }} 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

References

{{reflist}}

Further reading

{{refbegin | 2}}

  • {{cite journal | vauthors = Vanti WB, Nguyen T, Cheng R, Lynch KR, George SR, O'Dowd BF | title = Novel human G-protein-coupled receptors | journal = Biochemical and Biophysical Research Communications | volume = 305 | issue = 1 | pages = 67–71 | date = May 2003 | pmid = 12732197 | doi = 10.1016/S0006-291X(03)00709-5 }}
  • {{cite journal | vauthors = Ottolenghi C, Fellous M, Barbieri M, McElreavey K | title = Novel paralogy relations among human chromosomes support a link between the phylogeny of doublesex-related genes and the evolution of sex determination | journal = Genomics | volume = 79 | issue = 3 | pages = 333–343 | date = March 2002 | pmid = 11863363 | doi = 10.1006/geno.2002.6711 }}
  • {{cite journal | vauthors = Takeda S, Kadowaki S, Haga T, Takaesu H, Mitaku S | title = Identification of G protein-coupled receptor genes from the human genome sequence | journal = FEBS Letters | volume = 520 | issue = 1–3 | pages = 97–101 | date = June 2002 | pmid = 12044878 | doi = 10.1016/S0014-5793(02)02775-8 | s2cid = 7116392 | doi-access = }}
  • {{cite journal | vauthors = Gloriam DE, Schiöth HB, Fredriksson R | title = Nine new human Rhodopsin family G-protein coupled receptors: identification, sequence characterisation and evolutionary relationship | journal = Biochimica et Biophysica Acta (BBA) - General Subjects | volume = 1722 | issue = 3 | pages = 235–246 | date = April 2005 | pmid = 15777626 | doi = 10.1016/j.bbagen.2004.12.001 }}
  • {{cite journal | vauthors = Matsuo A, Matsumoto S, Nagano M, Masumoto KH, Takasaki J, Matsumoto M, Kobori M, Katoh M, Shigeyoshi Y | display-authors = 6 | title = Molecular cloning and characterization of a novel Gq-coupled orphan receptor GPRg1 exclusively expressed in the central nervous system | journal = Biochemical and Biophysical Research Communications | volume = 331 | issue = 1 | pages = 363–369 | date = May 2005 | pmid = 15845401 | doi = 10.1016/j.bbrc.2005.03.174 }}

{{refend}}

{{G protein-coupled receptors}}

Category:G protein-coupled receptors

{{transmembranereceptor-stub}}