ArticleEndocrinology2013
A novel experimental strategy to assess the metabolic effects of selective activation of a G(q)-coupled receptor in hepatocytes in vivo.
Article in Endocrinology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 41 papers.
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Who cites it
41 citing papers in PubMed, 69 citations in OpenAlex.
- Copeptin and Estimated Insulin Sensitivity in Adults With and Without Type 1 Diabetes: The CACTI Study.Canadian journal of diabetes · 2019Trial
- Overview of the DREADDs chemogenetics and the patent landscape of their actuators.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Review
- Correlation of G protein-coupled receptor and tumor microenvironment with gastric cancer outcomes and therapies.Chinese medical journal · 2026Article
- A humanized Gs-coupled DREADD for circuit and behavior modulation.Frontiers in cellular neuroscience · 2025Article
- Article
- GNature communications · 2024Article
- G protein selectivity profile of GPR56/ADGRG1 and its effect on downstream effectors.Research square · 2024Article
- G protein selectivity profile of GPR56/ADGRG1 and its effect on downstream effectors.Cellular and molecular life sciences : CMLS · 2024Article
- Identification of GαScientific reports · 2024Article
- Multi-omics identification of GPCR gene features in lung adenocarcinoma based on multiple machine learning combinations.Journal of Cancer · 2024Article
- Review
- Screening of Biomarkers in Liver Tissue after Bariatric Surgery Based on WGCNA and SVM-RFE Algorithms.Disease markers · 2023Article
- Mapping and targeted viral activation of pancreatic nerves in mice reveal their roles in the regulation of glucose metabolism.Nature biomedical engineering · 2022Article
- GLP1R inhibits the progression of endometrial carcinoma through activation of cAMP/PKA pathway.Journal of clinical laboratory analysis · 2022Article
- Targeted Activation of G-Protein Coupled Receptor-Mediated CaTissue engineering. Part A · 2022Article
- Review
- GPR21 Inhibition Increases Glucose-Uptake in HepG2 Cells.International journal of molecular sciences · 2021Article
- Chemogenetic approaches to identify metabolically important GPCR signaling pathways: Therapeutic implications.Journal of neurochemistry · 2021Review
- Vasopressin mediates fructose-induced metabolic syndrome by activating the V1b receptor.JCI insight · 2021Article
- Designer GPCRs as Novel Tools to Identify Metabolically Important Signaling Pathways.Frontiers in endocrinology · 2021Article
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11 authors at 2 institutions in 1 country.
Funding
Abstract
Increased hepatic glucose production is a key pathophysiological feature of type 2 diabetes. Like all other cell types, hepatocytes express many G protein-coupled receptors (GPCRs) that are linked to different functional classes of heterotrimeric G proteins. The important physiological functions mediated by G(s)-coupled hepatic glucagon receptors are well-documented. In contrast, little is known about the in vivo physiological roles of hepatocyte GPCRs that are linked to G proteins of the G(q) family. To address this issue, we established a transgenic mouse line (Hep-Rq mice) that expressed a G(q)-linked designer receptor (Rq) in a hepatocyte-selective fashion. Importantly, Rq could no longer bind endogenous ligands but could be selectively activated by a synthetic drug, clozapine-N-oxide. Clozapine-N-oxide treatment of Hep-Rq mice enabled us to determine the metabolic consequences caused by selective activation of a G(q)-coupled GPCR in hepatocytes in vivo. We found that acute Rq activation in vivo led to pronounced increases in blood glucose levels, resulting from increased rates of glycogen breakdown and gluconeogenesis. We also demonstrated that the expression of the V(1b) vasopressin receptor, a G(q)-coupled receptor expressed by hepatocytes, was drastically increased in livers of ob/ob mice, a mouse model of diabetes. Strikingly, treatment of ob/ob mice with a selective V(1b) receptor antagonist led to reduced glucose excursions in a pyruvate challenge test. Taken together, these findings underscore the importance of G(q)-coupled receptors in regulating hepatic glucose fluxes and suggest novel receptor targets for the treatment of type 2 diabetes.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.