mProX™ Human GPR139 Stable Cell Line

Product Information

Target Family

Orphan Family

Target Protein Species

Human

Host Cell Type

CHO-K1;HEK293

Target Classification

Other Targets Drug Discovery Assays and Products

Target Research Area

CNS Research;Metabolic Research

Related Diseases

Adult-Onset Severe Asthma;Isolated Growth Hormone Deficiency, Type Ib

Gene ID

Human:124274

UniProt ID

Human:Q6DWJ6

Product Properties

Biosafety Level

Level 1

Activity

Yes

Quantity

10⁶ cells per vial

Applications

GPR139 is a neuromodulatory orphan receptor that has been associated with various neuropsychiatric behaviors. Recent studies have shown that loss of GPR139 in mice results in neuropsychiatric manifestations, including increased anxiety-related traits and social interaction deficits, suggesting schizophrenia-like symptoms. Moreover, GPR139 has been linked to the regulation of body mass, blood glucose, and insulin, indicating its potential role in metabolic disorders. The recent discovery of TAK-041, a potent and selective GPR139 agonist, has further highlighted the therapeutic potential of targeting GPR139 for the treatment of negative symptoms associated with schizophrenia.

Protocols

Please visit our protocols page.

Customer Reviews

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FAQ

chat Ronald (Verified Customer)

How is GPR139 associated with fear learning in zebrafish? Nov 18 2021

chat Patrick Liam (Creative Biolabs Scientific Support)

GPR139 is an evolutionarily conserved orphan receptor predominantly expressed in the habenula of vertebrate species. Research suggests that activation of GPR139 signaling in the habenula may be involved in fear learning processes in zebrafish. Nov 18 2021

chat Paul (Verified Customer)

What is the significance of the orphan GPR139 G protein-coupled receptor? Jul 24 2020

chat Patrick Liam (Creative Biolabs Scientific Support)

GPR139 is an orphan G protein-coupled receptor. While its endogenous agonists are not firmly established, aromatic amino acids L-Trp and L-Phe have been shown to activate it. This receptor has potential implications in metabolic disorders and Parkinson's disease. Jul 24 2020

Published Data

Fig.1 In CHO-K1 cells stably expressing GPR139, a ligand found in brain extracts induces Ca²⁺ mobilization.

Transiently transfected CHO-K1 cells stably expressing GPR139 or SALPR as a control were transfected with vectors coding for apoaequorin as a Ca²⁺ sensor and Ga16 to improve signaling. The Ca²⁺-induced bioluminescence is provided in relative light units (RLU) after subtracting the basal medium response. Incubation in a peptide-enriched extract from porcine brain boosted Ca²⁺ mobilization in a dose-dependent manner. The concentration of the brain extract is given in arbitrary units (AU) based on the dilutions. For each concentration, the findings are averaged over three to six independent measurements and shown as means ± SD.

Ref: Süsens, Ute, et al. "Characterisation and differential expression of two very closely related G-protein-coupled receptors, GPR139 and GPR142, in mouse tissue and during mouse development." Neuropharmacology 50.4 (2006): 512-520.

Pubmed: 16378626

DOI: 10.1016/j.neuropharm.2005.11.003

Research Highlights

Yao Lu et al. "Molecular insights into orphan G protein-coupled receptors relevant to schizophrenia." British journal of pharmacology, 22 Aug. 2023
The study examines the potential for GPR3, GPR6, GPR12, GPR52, GPR85, GPR88, and GPR139 as therapeutic targets for schizophrenia. The researchers provide an overview of the expression, signal mechanisms, and cellular roles of these receptors, along with developments in small molecule therapies and structural understanding. This analysis aims to showcase the increasing evidence and potential for novel treatments for schizophrenia utilizing these G protein-coupled receptors. The paper aims to offer a concise summary of the current state of research on this topic.
Yao Lu et al. "Molecular insights into orphan G protein-coupled receptors relevant to schizophrenia." British journal of pharmacology, 22 Aug. 2023
Pubmed: 37605621 DOI: 10.1111/bph.16221

Lisa Pallareti et al. "Pharmacological characterization of novel small molecule agonists and antagonists for the orphan receptor GPR139." European journal of pharmacology, 15 Mar. 2023
In their study, the authors investigated the efficacy of JNJ-63533054-mediated signaling and internalization compared to Compound 1a. Virtual screening for GPR139 agonists and antagonists was then conducted and validated in functional assays. Results showed four GPR139 agonists, with similar or reduced potency to known compounds. Likewise, GPR139 agonist and antagonist analogs identified through substructure searches behaved similarly to their parent compounds. The study provides new insights and potential tools for future medical chemistry studies.
Lisa Pallareti et al. "Pharmacological characterization of novel small molecule agonists and antagonists for the orphan receptor GPR139." European journal of pharmacology, 15 Mar. 2023
Pubmed: 36736525 DOI: 10.1016/j.ejphar.2023.175553