<i>GPR52</i> | Class A Orphans | IUPHAR/BPS Guide to PHARMACOLOGY

GPR52

Target id: 108

Nomenclature: GPR52

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

   GtoImmuPdb view: OFF :     Currently no data for GPR52 in GtoImmuPdb

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 361 1q24 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
Specialist databases
GPCRDB gpr52_human (Hs), gpr52_mouse (Mm)
Other databases
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 Affinity Units Reference
derivative 17 [Nakahata et al., 2018] Hs Agonist 7.7 pEC50 1
pEC50 7.7 (EC50 2.1x10-8 M) [1]
compound 7a [PMID: 24884590] Hs Agonist 7.6 pEC50 3
pEC50 7.6 (EC50 2.82x10-8 M) [3]
Tissue Distribution
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. Design and Synthesis of 1-(1-Benzothiophen-7-yl)-1H-Pyrazole, a Novel Series of G Protein-coupled Receptor 52 (GPR52) Agonists. Bioorganic & Medicinal Chemistry, In Press, Accepted Manuscript.

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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How to cite this page

Anthony P. Davenport, Stephen Alexander, Joanna L. Sharman, Adam J. Pawson, Helen E. Benson, Amy E. Monaghan, Wen Chiy Liew, Chido Mpamhanga, Jim Battey, Richard V. Benya, Robert T. Jensen, Sadashiva Karnik, Evi Kostenis, Eliot Spindel, Laura Storjohann, Kalyan Tirupula, Tom I. Bonner, Richard Neubig, Jean-Philippe Pin, Michael Spedding, Anthony Harmar.
Class A Orphans: GPR52. Last modified on 13/07/2018. Accessed on 19/11/2018. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=108.