<i>GPR142</i> | Class A Orphans | IUPHAR/BPS Guide to PHARMACOLOGY

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GPR142

Target not currently curated in GtoImmuPdb

Target id: 132

Nomenclature: GPR142

Family: Class A Orphans

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 462 17q23 GPR142 G protein-coupled receptor 142 1-2
Mouse 7 365 11 E2 Gpr142 G protein-coupled receptor 142 1-2
Rat 7 - 10q32.2 Gpr142 G protein-coupled receptor 142
Previous and Unofficial Names
KIF19 | AXOR103 | G-protein coupled receptor PGR2
Database Links
Specialist databases
GPCRDB gp142_human (Hs), gp142_mouse (Mm)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
compound 33 [Toda et al., 2013] Hs Agonist 7.7 pEC50 3
pEC50 7.7 (EC50 2.2x10-8 M) [3]
Agonist Comments
The high identity of 50% between GPR142 and GPR139 is suggestive of shared ligands [2].
Tissue Distribution
Brain (intense labeling of hippocampus, dentate gyrus, cerebral cortex, medial thalamic nuclei, anterior hypothalamic nuclei), thymus, liver, cartilage
Species:  Mouse
Technique:  In situ hybridization
References:  2
Spleen, liver, kidney, testis, brain
Species:  Mouse
Technique:  Multi-tissue cDNA panel (PCR)
References:  2
Tissue Distribution Comments
Embryonic expression of GPR142 suggests the receptor may play a role in brain, bone and blood formation [2].
Expression Datasets

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Biologically Significant Variants
Type:  Single nucleotide polymorphism
Species:  Human
Amino acid change:  R86H
Global MAF (%):  1
Subpopulation MAF (%):  ASN: 3
Minor allele count:  A=0.007/16
Comment on frequency:  Low frequency (<10% in all tested populations)
SNP accession: 
Validation:  1000 Genomes, Frequency
Type:  Single nucleotide polymorphism
Species:  Human
Amino acid change:  H132D
Global MAF (%):  3
Subpopulation MAF (%):  AFR|AMR: 12|3
Minor allele count:  C=0.032/70
SNP accession: 
Validation:  1000 Genomes, Frequency
Type:  Single nucleotide polymorphism
Species:  Human
Amino acid change:  R124Q
Global MAF (%):  1
Subpopulation MAF (%):  AFR: 3
Minor allele count:  A=0.006/14
Comment on frequency:  Low frequency (<10% in all tested populations)
SNP accession: 
Validation:  1000 Genomes, Frequency

References

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1. Fredriksson R, Höglund PJ, Gloriam DE, Lagerström MC, Schiöth HB. (2003) Seven evolutionarily conserved human rhodopsin G protein-coupled receptors lacking close relatives. FEBS Lett., 554 (3): 381-8. [PMID:14623098]

2. Süsens U, Hermans-Borgmeyer I, Urny J, Schaller HC. (2006) Characterisation and differential expression of two very closely related G-protein-coupled receptors, GPR139 and GPR142, in mouse tissue and during mouse development. Neuropharmacology, 50 (4): 512-20. [PMID:16378626]

3. Toda N, Hao X, Ogawa Y, Oda K, Yu M, Fu Z, Chen Y, Kim Y, Lizarzaburu M, Lively S et al.. (2013) Potent and Orally Bioavailable GPR142 Agonists as Novel Insulin Secretagogues for the Treatment of Type 2 Diabetes. ACS Med Chem Lett, 4 (8): 790-4. [PMID:24900747]

Contributors

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