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  • mProX™ Human GPR146 Stable Cell Line

    [CAT#: S01YF-1023-PY309]
    Product Category:
    Membrane Protein Stable Cell Lines
    Subcategory:

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    Product Information

    Target Family
    Orphan Family
    Target Protein Species
    Human
    Host Cell Type
    KATO;III;CHO-K1;HEK293
    Target Classification
    Other Targets Drug Discovery Assays and Products
    Gene ID
    Human:115330
    UniProt ID
    Human:Q96CH1

    Product Properties

    Biosafety Level
    Level 1
    Activity
    Yes
    Quantity
    10⁶ cells per vial
    Applications
    GPR146, a G Protein-Coupled Receptor, has recently been associated with cholesterol metabolism. Studies have shown that hypercholesterolemia risk-associated GPR146 regulates blood cholesterol levels in both humans and mice. Furthermore, GPR146 variants have been linked to a beneficial cardiometabolic risk profile, suggesting its potential as a therapeutic target for atherosclerosis and related conditions. The emerging research on GPR146 underscores its significance in maintaining cholesterol homeostasis and its potential implications for cardiovascular health.

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    FAQ

    chat Melissa (Verified Customer)

    How does GPR146 deficiency impact hypercholesterolemia and atherosclerosis? Apr 29 2021

    chat Patrick Liam (Creative Biolabs Scientific Support)

    GPR146 deficiency has been shown to provide protection against hypercholesterolemia and atherosclerosis. Remarkably, GPR146-deficient mice exhibited reduced plasma cholesterol levels and a significant decrease in aortic atherosclerotic lesions. Apr 29 2021

    chat Ronald (Verified Customer)

    Is GPR146 a potential therapeutic target for cholesterol homeostasis? Aug 29 2022

    chat Patrick Liam (Creative Biolabs Scientific Support)

    Yes, GPR146 has emerged as a potential therapeutic target for achieving cholesterol homeostasis. Genome-wide association studies have linked GPR146 to human atherosclerosis, and its influence on serum cholesterol homeostasis has been described in recent research. Aug 29 2022

    Published Data

    Fig.1 GPR146 knockdown fully inhibited C-peptide's ability to trigger cFos expression in KATO III cells.

    In the experiment, when KATOIII cells were transfected with vehicle (Lipofectamine alone, without siRNA), control siRNA (targeting green fluorescent protein, eGFP), or siRNA specific to GPR107 or GPR160, no significant changes were observed in C-peptide-induced cFos expression. Surprisingly, silencing GPR146 had a remarkable effect, rendering KATOIII cells unresponsive to C-peptide exposure.

    Ref: Yosten, Gina LC, et al. "Evidence for an interaction between proinsulin C-peptide and GPR146." Journal of Endocrinology 218.2 (2013): B1-B8.

    Pubmed: 23759446

    DOI: 10.1530/JOE-13-0203

    Research Highlights

    Isabell Kaczmarek et al. "Identifying G protein-coupled receptors involved in adipose tissue function using the innovative RNA-seq database FATTLAS." iScience, 20 Oct. 2023
    The effect of G protein-coupled receptors (GPCRs) on adipose tissue (AT) and adipocytes has been extensively studied. However, the specific repertoire, regulation and function of GPCRs in conditions such as obesity, remains unclear. To address this gap, a new interactive public database called FATTLAS has been established for improved access and analysis of RNA-seq data from mouse and human AT. Through the extraction and analysis of GPCRome from non-obese and obese individuals, highly expressed and differentially regulated GPCRs were identified. Four GPCRs (GPR146, MRGPRF, FZD5, PTGER2) were found to be involved in adipogenesis and were further studied in a (pre)adipocyte cell model. Of these, MRGPRF was essential for adipocyte viability and regulating cAMP levels, while GPR146 was seen to modulate adipocyte lipolysis through constitutive activation of Gi proteins. By utilizing FATTLAS, this study has identified and described four previously unrecognized GPCRs associated with AT function and adipogenesis.
    Isabell Kaczmarek et al. "Identifying G protein-coupled receptors involved in adipose tissue function using the innovative RNA-seq database FATTLAS." iScience, 20 Oct. 2023
    Pubmed: 37766984   DOI: 10.1016/j.isci.2023.107841

    Juliette A de Klerk et al. "Altered blood gene expression in the obesity-related type 2 diabetes cluster may be causally involved in lipid metabolism: a Mendelian randomisation study." Diabetologia, 2023
    The aim of this study was to identify differentially expressed lncRNAs and mRNAs in whole blood samples from individuals with type 2 diabetes who were categorized into five distinct clusters: severe insulin-deficient diabetes (SIDD), severe insulin-resistant diabetes (SIRD), mild obesity-related diabetes (MOD), mild diabetes (MD), and mild diabetes with high HDL-cholesterol (MDH). This research aimed to enhance the understanding of the molecular mechanisms underlying these five different clusters of type 2 diabetes. Through the use of RNA sequencing, differentially expressed genes were identified in each cluster, and further validation was performed through the Innovative Medicines Initiative DIabetes REsearCh on patient straTification (IMI DIRECT) study. Additionally, to examine the potential causal effects of these genes on various diabetes-related traits, a two-sample Mendelian randomisation analysis was conducted using publicly available genome-wide association study (GWAS) data. The MOD cluster showed 11 differentially expressed lncRNAs and 175 mRNAs, while the SIDD and MDH clusters displayed upregulated lncRNA AL354696.2 and downregulated GPR15 mRNA, respectively. Correlations were observed among the differentially expressed genes in the MOD cluster. Through validation in the IMI DIRECT study, six lncRNAs and 120 mRNAs were found to be differentially expressed. Furthermore, the Mendelian randomisation analysis revealed 52 mRNAs with a potential causal effect on various anthropometric and lipid metabolism traits, including GPR146, which showed a causal effect on HDL-cholesterol levels without evidence of reverse causality. These findings highlight the role of lncRNAs and mRNAs in individuals with type 2 diabetes, particularly in the MOD cluster, and their potential impact on different diabetes-relevant traits.
    Juliette A de Klerk et al. "Altered blood gene expression in the obesity-related type 2 diabetes cluster may be causally involved in lipid metabolism: a Mendelian randomisation study." Diabetologia, 2023
    Pubmed: 36826505   DOI: 10.1007/s00125-023-05886-8

    Please note: All products are "FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC OR CLINICAL PROCEDURES" For licensing inquiries, please contact
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