GPR52 Membrane Protein Introduction

Introduction of GPR52

GPR52 is a protein encoded by the human GPR52 gene. It belongs to the G protein-coupled receptor (GPR) family which plays important roles in signal transduction from the external environment to the inside of the cell. It was first reported as a novel human gene identified by performing homology searches. During the past years, GPR52 has been widely researched for its functions and applications.

Function of GPR52 Membrane Protein

The GPCR family plays an important role in signal transduction from the external environment to the inside of the cell thus regulating intracellular signaling and gene expression. This receptor family responds to a broad spectrum of extracellular ligands, including nucleotides, peptides, biogenic amines, glycoprotein hormones or light, and amplifies the signal inside the cell by interacting with heterotrimeric GTP-binding proteins. As a member of the GPCR family, GPR52 shares the characteristic structural motif of seven transmembrane TM domains. Studies have shown that GPR52 is predominantly expressed in the brain, with the highest expression levels in the striatum and nucleus accumbens (NAc), which have been implicated in psychosis. Furthermore, GPR52 is also clearly detected in critical brain regions that are involved in cognitive functions, including the prefrontal cortex, entorhinal cortex, cingulate cortex, and mammillary nucleus. Recently, GPR52 has been proposed as a potential therapeutic target for schizophrenia. Most importantly, many agonists of GPR52 have been found to provide new therapeutic options for the treatment of positive and cognitive symptoms of schizophrenia.

Fig.1 Striatal-enriched GPCRs in medium-sized spiny neurons (MSNs) in striatum. (Komatsu, 2015)

Application of GPR52 Membrane Protein in Literature

1. Nishiyama K., et.al. 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 research. 2017, 1670:24-31. PubMed ID: 28583861
   
   

   This article reveals that GPR52 may play a role in modulating the function of striatopallidal neurons, possibly by interaction of GPR52 with ADORA2A and DRD2.

2. Komatsu H., et.al. Anatomical transcriptome of G protein-coupled receptors leads to the identification of a novel therapeutic candidate GPR52 for psychiatric disorders. PloS one. 2014, 9(2):e90134. PubMed ID: 24587241
   
   

   This article suggests that GPR52 may modulate dopaminergic and glutamatergic transmission in neuronal circuits responsible for cognitive function and emotion. GPR52 knockout and transgenic mice exhibit psychosis-related and antipsychotic-like behaviors. It indicates that GPR52 has the potential of being a therapeutic psychiatric receptor.

3. Song H., et.al. Targeting Gpr52 lowers mutant HTT levels and rescues Huntington’s disease-associated phenotypes. Brain. 2018, 141(6):1782-98. PubMed ID: 29608652
   
   

   This article suggests that knocking-out GPR52 significantly could reduce mutant HTT levels in the striatum and rescue Huntington's disease-associated behavioral phenotypes in a knock-in Huntington's disease mouse model. It indicates that Gpr52 may be a potential drug target for Huntington's disease.

4. Nakahata T., et.al. Design and synthesis of 1-(1-benzothiophene-7-yl)-1H-pyrazole, a novel series of G protein-coupled receptor 52 (GPR52) agonists. Bioorganic & medicinal chemistry. 2018, 26(8):1598-608. PubMed ID: 29478803
   
   

   This article identifies 3-methyl-5-hydroxymethyl-1H-pyrazole derivative 17 with potent GPR52 agonistic activity and good solubility. Furthermore, this compound 17 dose-dependently suppresses methamphetamine-induced hyperlocomotion in mice.

5. Nishiyama K., et.al. FTBMT, a Novel and Selective GPR52 Agonist, Demonstrates Antipsychotic-Like and Procognitive Effects in Rodents, Revealing a Potential Therapeutic Agent for Schizophrenia. Journal of Pharmacology and Experimental Therapeutics. 2017, 363(2):253-64. PubMed ID: 28851764
   
   

   This article suggests that FTBMT, a novel GPR52 agonist, has antipsychotic and recognitive properties without causing catalepsy in rodents. And it may be used as a new therapeutic option for the treatment of positive and cognitive symptoms of schizophrenia.

GPR52 Preparation Options

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Reference

1. Komatsu H. (2015). Novel therapeutic GPCRs for psychiatric disorders. International journal of molecular sciences. 16(6), 14109-14121.

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