G-protein coupled receptor 139 (GPC139) is a protein that in humans is encoded by the GPR139gene.[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]
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.
^ abcGRCh38: Ensembl release 89: ENSG00000180269 - Ensembl, May 2017
^ abcGRCm38: 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. PMC153653. 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. PMC8882194. 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.
Further readingedit
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.
gpr139, protein, coupled, receptor, gpc139, protein, that, humans, encoded, gene, research, shown, that, mice, with, loss, gcp139, experience, schizophrenia, like, symptomatology, that, rescued, with, dopamine, receptor, antagonist, haloperidol, opioid, recept. 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 m opioid receptor antagonist naltrexone 7 8 GPR139IdentifiersAliasesGPR139 GPRg1 PGR3 G protein coupled receptor 139External IDsOMIM 618448 MGI 2685341 HomoloGene 45860 GeneCards GPR139Gene location Human Chr Chromosome 16 human 1 Band16p12 3Start20 028 239 bp 1 End20 073 890 bp 1 Gene location Mouse Chr Chromosome 7 mouse 2 Band7 7 F2Start118 739 970 bp 2 End118 783 826 bp 2 RNA expression patternBgeeHumanMouse ortholog Top expressed incaudate nucleusputamennucleus accumbenshypothalamusbone marrowsubstantia nigrapituitary glandmuscle tissuesmooth muscle tissueendometriumTop expressed inhabenulamedial vestibular nucleusmammillary bodydorsal tegmental nucleusdorsomedial hypothalamic nucleuslateral hypothalamuscarotid bodyventral tegmental areaglobus pallidusparaventricular nucleus of hypothalamusMore reference expression dataBioGPSMore reference expression dataGene ontologyMolecular functionG protein coupled receptor activity protein dimerization activity signal transducer activity neuropeptide receptor activityCellular componentintegral component of membrane plasma membrane membraneBiological processG protein coupled receptor signaling pathway phospholipase C activating G protein coupled receptor signaling pathway neuropeptide signaling pathway signal transductionSources Amigo QuickGOOrthologsSpeciesHumanMouseEntrez124274209776EnsemblENSG00000180269ENSMUSG00000066197UniProtQ6DWJ6Q80UC8RefSeq mRNA NM 001002911NM 001318483NM 001024138RefSeq protein NP 001002911NP 001305412NP 001019309Location UCSC Chr 16 20 03 20 07 MbChr 7 118 74 118 78 MbPubMed search 3 4 WikidataView Edit HumanView Edit MouseLigands editAgonistsZelatriazin 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 AntagonistsJNJ 3792165References edit 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 Nohr AC Gloriam DE Brauner 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 Further reading editVanti 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 Schioth 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 nbsp This transmembrane receptor related article is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title GPR139 amp oldid 1191395022, wikipedia, wiki, book, books, library,
