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GPR52

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Target not currently curated in GtoImmuPdb

Target id: 108

Nomenclature: GPR52

Family: Class A Orphans

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 361 1q25.1 GPR52 G protein-coupled receptor 52 2
Mouse 7 361 1 H2.1 Gpr52 G protein-coupled receptor 52
Rat 7 361 13q22 Gpr52 G protein-coupled receptor 52
Database Links Click here for help
Specialist databases
GPCRDB gpr52_human (Hs), gpr52_mouse (Mm)
Other databases
ChEMBL Target CHEMBL3297639 (Hs), CHEMBL4105791 (Mm)
Ensembl Gene ENSG00000203737 (Hs)
Entrez Gene 9293 (Hs), 620246 (Mm), 680192 (Rn)
Human Protein Atlas ENSG00000203737 (Hs)
KEGG Gene hsa:9293 (Hs), mmu:620246 (Mm), rno:680192 (Rn)
OMIM 604106 (Hs)
Pharos Q9Y2T5 (Hs)
RefSeq Nucleotide NM_005684 (Hs), NM_001146330 (Mm)
RefSeq Protein NP_005675 (Hs), NP_001139802 (Mm)
UniProtKB Q9Y2T5 (Hs), P0C5J4 (Mm)
Wikipedia GPR52 (Hs)

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
derivative 17 [Nakahata et al., 2018] Small molecule or natural product Ligand has a PDB structure Hs Agonist 7.7 pEC50 1
⤷ pEC50 7.7 (EC50 2.1x10-8 M) [1]
compound 7a [PMID: 24884590] Small molecule or natural product Hs Agonist 7.6 pEC50 3
⤷ pEC50 7.6 (EC50 2.82x10-8 M) [3]
Tissue Distribution Click here for help
Caudate and putamen region of brain
Species:  Human
Technique:  Northern blot
References:  2
General Comments
GPR52 has four potential N-linked glysosylation sites, five PKA/PKC and six PKC intracellular phosphorylation sites and three putative C-tail palmitoylation sites [2].

References

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1. Nakahata T, Tokumaru K, Ito Y, Ishii N, Setoh M, Shimizu Y, Harasawa T, Aoyama K, Hamada T, Kori M et al.. (2018) Design and synthesis of 1-(1-benzothiophen-7-yl)-1H-pyrazole, a novel series of G protein-coupled receptor 52 (GPR52) agonists. Bioorg Med Chem, 26 (8): 1598-1608. [PMID:29478803]

2. Sawzdargo M, Nguyen T, Lee DK, Lynch KR, Cheng R, Heng HH, George SR, O'Dowd BF. (1999) Identification and cloning of three novel human G protein-coupled receptor genes GPR52, PsiGPR53 and GPR55: GPR55 is extensively expressed in human brain. Brain Res Mol Brain Res, 64 (2): 193-8. [PMID:9931487]

3. Setoh M, Ishii N, Kono M, Miyanohana Y, Shiraishi E, Harasawa T, Ota H, Odani T, Kanzaki N, Aoyama K et al.. (2014) Discovery of the first potent and orally available agonist of the orphan G-protein-coupled receptor 52. J Med Chem, 57 (12): 5226-37. [PMID:24884590]

Contributors

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