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Updated: May 4, 2026

Homogeneous Time-resolved Förster Resonance Energy Transfer-based Assay for Detection of Insulin Secretion
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Homogeneous Time-resolved Förster Resonance Energy Transfer-based Assay for Detection of Insulin Secretion

Published on: May 10, 2018

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GPRC5B a putative glutamate-receptor candidate is negative modulator of insulin secretion

Arvind Soni, Stefan Amisten, Patrik Rorsman

    Biochemical and Biophysical Research Communications
    |January 10, 2014
    PubMed

    Insights

    Increased G protein-coupled receptor 5B (GPRC5B) expression in pancreatic islets is linked to type 2 diabetes. Lowering GPRC5B levels improves insulin secretion and beta-cell survival, suggesting it as a therapeutic target.

    Area of Science:

    • Endocrinology
    • Molecular Biology
    • Diabetes Research

    Background:

    • G protein-coupled receptor 5B (GPRC5B) is a member of the GPCR group C family.
    • GPRC5B is highly expressed in pancreatic islets and its levels are elevated in type 2 diabetes.
    • GPRC5B expression is developmentally regulated, being lower in newborn than adult mice.

    Purpose of the Study:

    • To investigate the role of GPRC5B in pancreatic islet function and its potential involvement in type 2 diabetes.
    • To determine the effect of GPRC5B down-regulation on insulin secretion and beta-cell apoptosis.

    Main Methods:

    • Quantitative analysis of GPRC5B mRNA and protein expression in human and mouse pancreatic islets.
    • Lentiviral shRNA-mediated down-regulation of Gprc5b in mouse islets and MIN6 cells.
    • Measurement of insulin secretion under basal and stimulated conditions.
    • Assessment of cytokine-induced apoptosis in MIN6 cells.

    Main Results:

    • GPRC5B expression was 2.5-fold higher in islets from type 2 diabetes donors and significantly lower in newborn mice.
    • Gprc5b down-regulation in mouse islets strongly increased basal and potentiated glucose-stimulated insulin secretion.
    • Gprc5b down-regulation enhanced the effect of glutamate on insulin secretion and protected MIN6 cells from cytokine-induced apoptosis.

    Conclusions:

    • Elevated GPRC5B expression in pancreatic islets may contribute to reduced insulin secretion and beta-cell viability in type 2 diabetes.
    • Targeting GPRC5B pharmacologically presents a potential novel therapeutic strategy for type 2 diabetes treatment and prevention.

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