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Gene and Protein Information  |
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| 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 |
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| 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 
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| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Antagonists | |||||||||||||||||||||||||||||||||||||||||||||||||||
| Key to terms and symbols | View all chemical structures | Click column headers to sort | |||||||||||||||||||||||||||||||||||||||||||||||||
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| Tissue Distribution
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| 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]. |
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]
