Biology:GPR139

From HandWiki
Short description: Protein-coding gene in the species Homo sapiens


A representation of the 3D structure of the protein myoglobin showing turquoise α-helices.
Generic protein structure example

G-protein coupled receptor 139 (GPC139) is a protein that in humans is encoded by the GPR139 gene.[1][2] 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.[3][4]

Ligands

Agonists
  • Zelatriazin (TAK-41), (NBI-1065846) a potent, and GPR139 receptor selective agonist [5] 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

  1. ↑ "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. April 2003. doi:10.1073/pnas.0230374100. PMID 12679517. Bibcode: 2003PNAS..100.4903V. 
  2. ↑ "Entrez Gene: GPR139 G protein-coupled receptor 139". https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=124274. 
  3. ↑ "The role of orphan receptor GPR139 in neuropsychiatric behavior". Neuropsychopharmacology 47 (4): 902–913. March 2022. doi:10.1038/s41386-021-00962-2. PMID 33479510. 
  4. ↑ 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
  5. ↑ "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. August 2021. doi:10.1021/acs.jmedchem.1c00820. PMID 34260228. 

Further reading

  • "Novel human G-protein-coupled receptors". Biochemical and Biophysical Research Communications 305 (1): 67–71. May 2003. doi:10.1016/S0006-291X(03)00709-5. PMID 12732197. 
  • "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. March 2002. doi:10.1006/geno.2002.6711. PMID 11863363. 
  • "Identification of G protein-coupled receptor genes from the human genome sequence". FEBS Letters 520 (1–3): 97–101. June 2002. doi:10.1016/S0014-5793(02)02775-8. PMID 12044878. 
  • "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. April 2005. doi:10.1016/j.bbagen.2004.12.001. PMID 15777626. 
  • "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. May 2005. doi:10.1016/j.bbrc.2005.03.174. PMID 15845401. 



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