Top ▲

GtoPdb is requesting financial support from commercial users. Please see our sustainability page for more information.

GPR52

Click here for help

Target id: 108

Nomenclature: GPR52

Family: Class A Orphans with only surrogate ligands

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 4
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
Alphafold Q9Y2T5 (Hs), P0C5J4 (Mm)
ChEMBL Target CHEMBL3297639 (Hs), CHEMBL4105791 (Mm)
Ensembl Gene ENSG00000203737 (Hs), ENSMUSG00000118401 (Mm)
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]
NXE0041178 Small molecule or natural product Hs Agonist 7.6 pEC50 3
⤷ pEC50 7.6 (EC50 2.75x10-8 M) [3]
Description: Potency determined in a cAMP accumulation assay in HEK293F cells expressing hGPR52
compound 7a [PMID: 24884590] Small molecule or natural product Hs Agonist 7.6 pEC50 5
⤷ pEC50 7.6 (EC50 2.82x10-8 M) [5]
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
comp-43 Small molecule or natural product Hs Antagonist 6.2 pIC50 6
⤷ pIC50 6.2 (IC50 6.3x10-7 M) [6]
Tissue Distribution Click here for help
Caudate and putamen region of brain
Species:  Human
Technique:  Northern blot
References:  4
Physiological Consequences of Altering Gene Expression Comments
Genetic deletion elevated locomotor response to the A2A adenosine receptor antagonist istradefylline in mice [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 [4].

References

Show »

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. Nishiyama K, Suzuki H, Maruyama M, Yoshihara T, Ohta H. (2017) Genetic deletion of GPR52 enhances the locomotor-stimulating effect of an adenosine A2A receptor antagonist in mice: A potential role of GPR52 in the function of striatopallidal neurons. Brain Res, 1670: 24-31. [PMID:28583861]

3. Poulter S, Austin N, Armstrong R, Barnes M, Bucknell SJ, Higueruelo A, Banerjee J, Mead A, Mould R, MacSweeney C et al.. (2023) The Identification of GPR52 Agonist HTL0041178, a Potential Therapy for Schizophrenia and Related Psychiatric Disorders. ACS Med Chem Lett, 14 (4): 499-505. [PMID:37077397]

4. 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]

5. 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]

6. Wang C, Zhang YF, Guo S, Zhao Q, Zeng Y, Xie Z, Xie X, Lu B, Hu Y. (2021) GPR52 Antagonist Reduces Huntingtin Levels and Ameliorates Huntington's Disease-Related Phenotypes. J Med Chem, 64 (2): 941-957. [PMID:33185430]

How to cite this page