G protein-coupled receptors as regulators of pancreatic islet functionality.

Glucose homeostasis is maintained by hormones secreted from different types of pancreatic islets and its dysregulation can result in diseases including diabetes mellitus. The secretion of hormones from pancreatic islets is highly complex and tightly controlled by G protein-coupled receptors (GPCRs). Moreover, GPCR signaling may play a role in enhancing islet cell replication and proliferation. Thus, targeting GPCRs offers a promising strategy for regulating the functionality of pancreatic islets. Here, available RNAseq datasets from human and mouse islets were used to identify the GPCR expression profile and the impact of GPCR signaling for normal islet functionality is discussed.

• Publication year

  2022

• Venue

  Biochimica et biophysica acta. Molecular cell research

• Publication date

  2022-02-01

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.1016/j.bbamcr.2022.119235PMID 35151663
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Debates in Pancreatic Beta Cell Biology: Proliferation Versus Progenitor Differentiation and Transdifferentiation in Restoring β Cell Mass

  2021cited by this paper
• δ-Cells: The Neighborhood Watch in the Islet Community

  2021cited by this paper
• Glucagon Potentiates Insulin Secretion Via β-Cell GCGR at Physiological Concentrations of Glucose

  2021cited by this paper
• GIP mediates the incretin effect and glucose tolerance by dual actions on α cells and β cells

  2021cited by this paper
• Gsα-dependent signaling is required for postnatal establishment of a functional β-cell mass

  2021cited by this paper
• Silencing the G-protein coupled receptor 3-salt inducible kinase 2 pathway promotes human β cell proliferation

  2021cited by this paper
• Pharmacological blockade of the EP3 prostaglandin E2 receptor in the setting of type 2 diabetes enhances β-cell proliferation and identity and relieves oxidative damage

  2021cited by this paper
• Roles of GPRC5 family proteins: Focusing on GPRC5B and lipid-mediated signaling.

  2020cited by this paper
• Ghrelin suppresses insulin secretion in human islets and type 2 diabetes patients have diminished islet ghrelin cell number and lower plasma ghrelin levels.

  2020cited by this paper
• GPR120 regulates pancreatic polypeptide secretion from male mouse islets via PLC-mediated calcium mobilization.

  2020cited by this paper
• FFA2-, but not FFA3-agonists inhibit GSIS of human pseudoislets: a comparative study with mouse islets and rat INS-1E cells

  2020cited by this paper
• Global, regional, and national burden and trend of diabetes in 195 countries and territories: an analysis from 1990 to 2025

  2020cited by this paper
• Intra-islet glucagon signaling is critical for maintaining glucose homeostasis.

  2019cited by this paper
• Current status of GPR40/FFAR1 modulators in medicinal chemistry (2016–2019): a patent review

  2019cited by this paper
• Genetic basis of functional variability in adhesion G protein-coupled receptors

  2019cited by this paper
• Involvement of the Adhesion GPCRs Latrophilins in the Regulation of Insulin Release.

  2019cited by this paper
• β Cell tone is defined by proglucagon peptides through cAMP signaling.

  2019cited by this paper
• GPR40-Mediated Gα12 Activation by Allosteric Full Agonists Highly Efficacious at Potentiating Glucose-Stimulated Insulin Secretion in Human Islets

  2018cited by this paper
• G Protein-Coupled Receptors as Targets for Approved Drugs: How Many Targets and How Many Drugs?

  2018cited by this paper
• Trends in GPCR drug discovery: new agents, targets and indications

  2017cited by this paper
• Neuronal signals regulate obesity induced β-cell proliferation by FoxM1 dependent mechanism

  2017cited by this paper
• Single-cell transcriptomes identify human islet cell signatures and reveal cell-type–specific expression changes in type 2 diabetes

  2017cited by this paper
• Anti-diabetic action of all-trans retinoic acid and the orphan G protein coupled receptor GPRC5C in pancreatic β-cells.

  2017cited by this paper
• A comparative analysis of human and mouse islet G-protein coupled receptor expression

  2017cited by this paper
• Critical role for adenosine receptor A2a in β-cell proliferation

  2016cited by this paper
• β-arrestin drives MAP kinase signaling from clathrin-coated structures after GPCR dissociation

  2016cited by this paper
• Transcriptomic profiling of pancreatic alpha, beta and delta cell populations identifies delta cells as a principal target for ghrelin in mouse islets

  2016cited by this paper
• Neuronostatin acts via GPR107 to increase cAMP-independent PKA phosphorylation and proglucagon mRNA accumulation in pancreatic α-cells.

  2016cited by this paper
• G Protein-Coupled Receptor 119 (GPR119) Agonists for the Treatment of Diabetes: Recent Progress and Prevailing Challenges.

  2016cited by this paper
• Adhesion G Protein-Coupled Receptor G1 (ADGRG1/GPR56) and Pancreatic β-Cell Function.

  2016cited by this paper
• Novel Observations From Next-Generation RNA Sequencing of Highly Purified Human Adult and Fetal Islet Cell Subsets

  2015cited by this paper
• Alpha-, Delta- and PP-cells

  2015cited by this paper
• Pancreatic polypeptide regulates glucagon release through PPYR1 receptors expressed in mouse and human alpha-cells.

  2015cited by this paper
• Ghrelin

  2015cited by this paper
• Gαi/o-coupled receptor signaling restricts pancreatic β-cell expansion

  2015cited by this paper
• New insights into the architecture of the islet of Langerhans: a focused cross-species assessment

  2015cited by this paper
• Thrombin stimulates insulin secretion via protease-activated receptor-3

  2015cited by this paper
• Fetal endocannabinoids orchestrate the organization of pancreatic islet microarchitecture

  2015cited by this paper
• Urocortin3 mediates somatostatin-dependent negative feedback control of insulin secretion

  2015cited by this paper
• The transcriptional landscape of mouse beta cells compared to human beta cells reveals notable species differences in long non-coding RNA and protein-coding gene expression

  2014cited by this paper
• Control of Insulin Secretion by Cholinergic Signaling in the Human Pancreatic Islet

  2014cited by this paper
• Increased Perinatal Remodelling of the Pancreas in Somatostatin-Deficient Mice: Potential Role of Transforming Growth Factor-Beta Signalling in Regulating Beta Cell Growth in Early Life

  2014cited by this paper
• GIP contributes to islet trihormonal abnormalities in type 2 diabetes.

  2014cited by this paper
• Global genomic and transcriptomic analysis of human pancreatic islets reveals novel genes influencing glucose metabolism

  2014cited by this paper
• The G Protein-coupled Receptor P2Y14 Influences Insulin Release and Smooth Muscle Function in Mice*

  2014cited by this paper
• Distinctions between the islets of mice and men: implications for new therapies for type 1 and 2 diabetes.

  2013cited by this paper
• Prostaglandin E2 Receptor, EP3, Is Induced in Diabetic Islets and Negatively Regulates Glucose- and Hormone-Stimulated Insulin Secretion

  2013cited by this paper
• The Role of CXCL12-CXCR4 Signaling Pathway in Pancreatic Development

  2013cited by this paper
• Neuropeptide Y and somatostatin inhibit insulin secretion through different mechanisms.

  2013cited by this paper
• GPRC5B a putative glutamate-receptor candidate is negative modulator of insulin secretion.

  2013cited by this paper
• Inhibition of calcitonin gene-related peptide (CGRP) has the potential to extend first-phase insulin secretion.

  2013cited by this paper
• A Multiplexed Fluorescent Assay for Independent Second-Messenger Systems

  2013cited by this paper
• Cyclic AMP dynamics in the pancreatic β-cell

  2012cited by this paper
• Design and Functional Characterization of a Novel, Arrestin-Biased Designer G Protein-Coupled Receptor

  2012cited by this paper
• Understanding Molecular Recognition by G protein βγ Subunits on the Path to Pharmacological Targeting

  2011cited by this paper
• Characterization of Intestinal and Pancreatic Dysfunction in VPAC1-Null Mutant Mouse

  2011cited by this paper
• Stimulating beta cell replication and improving islet graft function by GPR119 agonists

  2011cited by this paper
• G Protein-Coupled Receptor Signaling and Sphingosine-1-Phosphate Play a Phylogenetically Conserved Role in Endocrine Pancreas Morphogenesis

  2011cited by this paper
• Systemic and acute administration of parathyroid hormone-related peptide(1–36) stimulates endogenous beta cell proliferation while preserving function in adult mice

  2011cited by this paper
• From the Cover: Ghrelin secretion stimulated by 1-adrenergic receptors in cultured ghrelinoma cells and in fasted mice

  2010cited by this paper
• Pancreas-specific Gsalpha deficiency has divergent effects on pancreatic alpha- and beta-cell proliferation.

  2010cited by this paper
• Pancreatic islet plasticity: Interspecies comparison of islet architecture and composition

  2010cited by this paper
• Noradrenaline inhibits exocytosis via the G protein βγ subunit and refilling of the readily releasable granule pool via the αi1/2 subunit

  2010cited by this paper
• M3-muscarinic receptor promotes insulin release via receptor phosphorylation/arrestin-dependent activation of protein kinase D1

  2010cited by this paper
• Serotonin Regulates Pancreatic β-Cell Mass during Pregnancy

  2010cited by this paper
• Regulation of Golgi structure and secretion by receptor-induced G protein βγ complex translocation

  2010cited by this paper
• Rgs16 and Rgs8 in embryonic endocrine pancreas and mouse models of diabetes

  2010cited by this paper
• A chemical-genetic approach to study G protein regulation of β cell function in vivo

  2009cited by this paper
• Somatostatin Secreted by Islet δ-Cells Fulfills Multiple Roles as a Paracrine Regulator of Islet Function

  2009cited by this paper
• Islet architecture: A comparative study

  2009cited by this paper
• Ghrelin-producing epsilon cells in the developing and adult human pancreas

  2009cited by this paper
• Beta cell-specific deficiency of the stimulatory G protein alpha-subunit Gsalpha leads to reduced beta cell mass and insulin-deficient diabetes.

  2007cited by this paper
• G12/13-dependent signaling of G-protein-coupled receptors: disease context and impact on drug discovery

  2007cited by this paper
• Characterization of somatostatin receptor subtype-specific regulation of insulin and glucagon secretion: an in vitro study on isolated human pancreatic islets.

  2007cited by this paper
• β cell-specific deficiency of the stimulatory G protein α-subunit Gsα leads to reduced β cell mass and insulin-deficient diabetes

  2007cited by this paper
• The role of alpha-cell dysregulation in fasting and postprandial hyperglycemia in type 2 diabetes and therapeutic implications.

  2007cited by this paper
• Blockade of Pancreatic Islet–Derived Ghrelin Enhances Insulin Secretion to Prevent High-Fat Diet–Induced Glucose Intolerance

  2006cited by this paper
• A critical role for beta cell M3 muscarinic acetylcholine receptors in regulating insulin release and blood glucose homeostasis in vivo.

  2006cited by this paper
• Endothelin inhibition delays onset of hyperglycemia and associated vascular injury in type I diabetes: evidence for endothelin release by pancreatic islet beta-cells.

  2005cited by this paper
• Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G-protein-coupled receptor.

  2005cited by this paper
• The GRAFS classification system of G-protein coupled receptors in comparative perspective.

  2005cited by this paper
• cAMP promotes pancreatic β-cell survival via CREB-mediated induction of IRS2

  2003cited by this paper
• cAMP promotes pancreatic beta-cell survival via CREB-mediated induction of IRS2.

  2003cited by this paper
• Free fatty acids regulate insulin secretion from pancreatic β cells through GPR40

  2003cited by this paper
• Signalling: Seven-transmembrane receptors

  2002cited by this paper
• Classical and new roles of β-arrestins in the regulation of G-PROTEIN-COUPLED receptors

  2001cited by this paper
• The insulinotropic effect of endothelin-1 is mediated by glucagon release from the islet alpha cells

  1999cited by this paper
• Pancreatic polypeptide secretion from the isolated perfused ventral and dorsal areas of the rat pancreas.

  1988cited by this paper

• Insulin Resistance and Inflammation

  2026cites this paper
• LGR4 is essential for maintaining β-cell homeostasis through suppression of RANK

  2025cites this paper
• Regulation of Type 1 Diabetes via Brown Adipocyte-Secreted Proteins and the Novel Glucagon Regulator Nidogen-2.

  2025cites this paper
• Intra-islet α-cell Gs signaling promotes glucagon release

  2024cites this paper
• SUCNR1 regulates insulin secretion and glucose elevates the succinate response in people with prediabetes

  2024cites this paper
• Commentary on “Intra‐islet α‐cell Gs signaling promotes glucagon release”

  2024cites this paper
• Comprehensive Search for GPCR Compounds which Can Enhance MafA and/or PDX-1 Expression Levels Using a Small Molecule Compound Library

  2023cites this paper
• The insulinotropic activity of oleosomes prepared from various sea buckthorn cultivars in mouse and human pancreatic β cell lines

  2023cites this paper
• The sympathetic nervous system in the 21st Century: neuro-immune interactions in metabolic homeostasis and obesity

  2022cites this paper
• Role of Reactive Oxygen Species in Glucose Metabolism Disorder in Diabetic Pancreatic β-Cells

  2022cites this paper