The Interplay of Glucagon-Like Peptide-1 Receptor Trafficking and Signalling in Pancreatic Beta Cells

Activation of the GLP-1 receptor by a non-peptidic agonist

(2020) Peishen Zhao et al.   NATURE

Super-resolution microscopy compatible fluorescent probes reveal endogenous glucagon-like peptide-1 receptor distribution and dynamics

(2020) Julia Ast et al.   Nature Communications

A kinetic method for measuring agonist efficacy and ligand bias using high resolution biosensors and a kinetic data analysis framework

(2020) Sam R. J. Hoare et al.   Scientific Reports

Signalling, trafficking and glucoregulatory properties of glucagon‐like peptide‐1 receptor agonists exendin‐4 and lixisenatide

(2020) Philip Pickford et al.   BRITISH JOURNAL OF PHARMACOLOGY

Brain Endothelial Cells Regulate Glucagon-Like Peptide 1 Entry Into the Brain via a Receptor-Mediated Process

(2020) Zhuo Fu et al.   Frontiers in Physiology

Endosome-to-TGN Trafficking: Organelle-Vesicle and Organelle-Organelle Interactions

(2020) Yingfeng Tu et al.   Frontiers in Cell and Developmental Biology

Pharmacological characterization of mono-, dual- and tri-peptidic agonists at GIP and GLP-1 receptors

(2020) Elita Yuliantie et al.   BIOCHEMICAL PHARMACOLOGY

Brain uptake pharmacokinetics of incretin receptor agonists showing promise as Alzheimer’s and Parkinson’s disease therapeutics

(2020) Therese S. Salameh et al.   BIOCHEMICAL PHARMACOLOGY

The Glycosphingolipid GM3 Modulates Conformational Dynamics of the Glucagon Receptor

(2020) T. Bertie Ansell et al.   BIOPHYSICAL JOURNAL

Discordance between GLP-1R gene and protein expression in mouse pancreatic islet cells

(2020) Sarah M Gray et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Disconnect between signalling potency and in vivo efficacy of pharmacokinetically optimised biased glucagon-like peptide-1 receptor agonists

(2020) Maria Lucey et al.   Molecular Metabolism

Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist

(2020) Francis S. Willard et al.   JCI Insight

Pathophysiology of Type 2 Diabetes Mellitus

(2020) Unai Galicia-Garcia et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Using a reporter mouse to map known and novel sites of GLP-1 receptor expression in peripheral tissues of male mice

(2020) Daniel B Andersen et al.   ENDOCRINOLOGY

Gs/Gq signaling switch in β cells defines incretin effectiveness in diabetes

(2020) Okechi S. Oduori et al.   JOURNAL OF CLINICAL INVESTIGATION

Endothelin-converting enzyme-1 regulates glucagon-like peptide-1 receptor signalling and resensitisation

(2019) Gary Brian Willars et al.   BIOCHEMICAL JOURNAL

Coming together to define membrane contact sites

(2019) Luca Scorrano et al.   Nature Communications

Biased Receptor Signaling in Drug Discovery

(2019) Terry Kenakin   PHARMACOLOGICAL REVIEWS

Mitochondrial interaction with the endosomal compartment in endocytosis and mitochondrial transfer

(2019) Kiran Todkar et al.   MITOCHONDRION

Towards a molecular understanding of endosomal trafficking by Retromer and Retriever

(2019) Kai‐En Chen et al.   TRAFFIC

β Cell–intrinsic β-arrestin 1 signaling enhances sulfonylurea-induced insulin secretion

(2019) Luiz F. Barella et al.   JOURNAL OF CLINICAL INVESTIGATION

New Insights into Beta-Cell GLP-1 Receptor and cAMP Signaling

(2019) Alejandra Tomas et al.   JOURNAL OF MOLECULAR BIOLOGY

Caveolae: The FAQs

(2019) Robert G. Parton et al.   TRAFFIC

Agonist-induced membrane nanodomain clustering drives GLP-1 receptor responses in pancreatic beta cells

(2019) Teresa Buenaventura et al.   PLOS BIOLOGY

Glucagon-like peptide 1 in health and disease

(2018) Andreas Andersen et al.   Nature Reviews Endocrinology

Mechanisms of clathrin-mediated endocytosis

(2018) Marko Kaksonen et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Targeting GLP-1 receptor trafficking to improve agonist efficacy

(2018) Ben Jones et al.   Nature Communications

Lack of beta-arrestin signaling in the absence of active G proteins

(2018) Manuel Grundmann et al.   Nature Communications

Glucagon-like peptide-1 receptor internalisation controls spatiotemporal signalling mediated by biased agonists

(2018) Madeleine M. Fletcher et al.   BIOCHEMICAL PHARMACOLOGY

Phase-plate cryo-EM structure of a biased agonist-bound human GLP-1 receptor–Gs complex

(2018) Yi-Lynn Liang et al.   NATURE

To degrade or not to degrade: mechanisms and significance of endocytic recycling

(2018) Peter J. Cullen et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Manifold roles of β-arrestins in GPCR signaling elucidated with siRNA and CRISPR/Cas9

(2018) Louis M. Luttrell et al.   Science Signaling

Efficacy and safety of LY3298176, a novel dual GIP and GLP-1 receptor agonist, in patients with type 2 diabetes: a randomised, placebo-controlled and active comparator-controlled phase 2 trial

(2018) Juan Pablo Frias et al.   LANCET

A role of PLC/PKC-dependent pathway in GLP-1-stimulated insulin secretion

(2017) Makoto Shigeto et al.   JOURNAL OF MOLECULAR MEDICINE-JMM

Single-molecule imaging reveals receptor–G protein interactions at cell surface hot spots

(2017) Titiwat Sungkaworn et al.   NATURE

Cryo-EM structure of the activated GLP-1 receptor in complex with a G protein

(2017) Yan Zhang et al.   NATURE

β-arrestin-2 is an essential regulator of pancreatic β-cell function under physiological and pathophysiological conditions

(2017) Lu Zhu et al.   Nature Communications

Gαs regulates Glucagon-Like Peptide 1 Receptor-mediated cyclic AMP generation at Rab5 endosomal compartment

(2017) Shravan Babu Girada et al.   Molecular Metabolism

Sensory Neurons that Detect Stretch and Nutrients in the Digestive System

(2016) Erika K. Williams et al.   CELL

iNKT Cells Induce FGF21 for Thermogenesis and Are Required for Maximal Weight Loss in GLP1 Therapy

(2016) Lydia Lynch et al.   Cell Metabolism

Actin-Sorting Nexin 27 (SNX27)-Retromer Complex Mediates Rapid Parathyroid Hormone Receptor Recycling

(2016) Jennifer C. McGarvey et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structural insight into antibody-mediated antagonism of the Glucagon-like peptide-1 Receptor

(2016) Stephanie Hennen et al.   Scientific Reports

Mechanism of allosteric regulation of β2-adrenergic receptor by cholesterol

(2016) Moutusi Manna et al.   eLife

Agonist-induced internalisation of the glucagon-like peptide-1 receptor is mediated by the Gαq pathway

(2015) Aiysha Thompson et al.   BIOCHEMICAL PHARMACOLOGY

Impact of Current and Emerging Glucose-Lowering Drugs on Body Weight in Type 2 Diabetes

(2015) David C.W. Lau et al.   Canadian Journal of Diabetes

Topical administration of GLP-1 receptor agonists prevents retinal neurodegeneration in experimental diabetes

(2015) Cristina Hernández et al.   DIABETES

Expression and Distribution of Glucagon-Like Peptide-1 Receptor mRNA, Protein and Binding in the Male Nonhuman Primate (Macaca mulatta) Brain

(2015) Kristy M. Heppner et al.   ENDOCRINOLOGY

GLP-1 stimulates insulin secretion by PKC-dependent TRPM4 and TRPM5 activation

(2015) Makoto Shigeto et al.   JOURNAL OF CLINICAL INVESTIGATION

Autocrine selection of a GLP-1R G-protein biased agonist with potent antidiabetic effects

(2015) Hongkai Zhang et al.   Nature Communications

Distribution and characterisation of Glucagon-like peptide-1 receptor expressing cells in the mouse brain

(2015) Simon C. Cork et al.   Molecular Metabolism

Involvement of cAMP/EPAC/TRPM2 Activation in Glucose- and Incretin-Induced Insulin Secretion

(2014) M. Yosida et al.   DIABETES

GLP-1 Receptor Localization in Monkey and Human Tissue: Novel Distribution Revealed With Extensively Validated Monoclonal Antibody

(2014) Charles Pyke et al.   ENDOCRINOLOGY

Functional Consequences of Glucagon-like Peptide-1 Receptor Cross-talk and Trafficking

(2014) Sarah Noerklit Roed et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The arcuate nucleus mediates GLP-1 receptor agonist liraglutide-dependent weight loss

(2014) Anna Secher et al.   JOURNAL OF CLINICAL INVESTIGATION

Endosomal generation of cAMP in GPCR signaling

(2014) Jean-Pierre Vilardaga et al.   Nature Chemical Biology

Spatial encoding of cyclic AMP signaling specificity by GPCR endocytosis

(2014) Nikoleta G Tsvetanova et al.   Nature Chemical Biology

Glucagon-like peptide-1 receptor-mediated endosomal cAMP generation promotes glucose-stimulated insulin secretion in pancreatic β-cells

(2013) Ramya S. Kuna et al.   AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM

Identification and Characterization of GLP-1 Receptor-Expressing Cells Using a New Transgenic Mouse Model

(2013) P. Richards et al.   DIABETES

Agonist-biased Trafficking of Somatostatin Receptor 2A in Enteric Neurons

(2013) Peishen Zhao et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Real-time trafficking and signaling of the glucagon-like peptide-1 receptor

(2013) Sarah Noerklit Roed et al.   MOLECULAR AND CELLULAR ENDOCRINOLOGY

Endoplasmic Reticulum Structure and Interconnections with Other Organelles

(2013) A. R. English et al.   Cold Spring Harbor Perspectives in Biology

Characterization of glucagon-like peptide 1 receptor (GLP1R) gene in chickens: functional analysis, tissue distribution, and identification of its transcript variants

(2012) G. Huang et al.   DOMESTIC ANIMAL ENDOCRINOLOGY

Anchored phosphatases modulate glucose homeostasis

(2012) Simon A Hinke et al.   EMBO JOURNAL

The Glucagon-Like Peptide-1 Receptor—or Not?

(2012) Charles Pyke et al.   ENDOCRINOLOGY

AP-3 regulates PAR1 ubiquitin-independent MVB/lysosomal sorting via an ALIX-mediated pathway

(2012) Michael R. Dores et al.   MOLECULAR BIOLOGY OF THE CELL

Molecular Mechanism of β-Arrestin-Biased Agonism at Seven-Transmembrane Receptors

(2011) Eric Reiter et al.   Annual Review of Pharmacology and Toxicology

A mTurquoise-Based cAMP Sensor for Both FLIM and Ratiometric Read-Out Has Improved Dynamic Range

(2011) Jeffrey B. Klarenbeek et al.   PLoS One

GLP-1 Mediates Antiapoptotic Effect by Phosphorylating Bad through a β-Arrestin 1-mediated ERK1/2 Activation in Pancreatic β-Cells

(2009) Julie Quoyer et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Sustained cyclic AMP production by parathyroid hormone receptor endocytosis

(2009) Sébastien Ferrandon et al.   Nature Chemical Biology

Persistent cAMP-Signals Triggered by Internalized G-Protein–Coupled Receptors

(2009) Davide Calebiro et al.   PLOS BIOLOGY

Role of the cAMP sensor Epac as a determinant of KATPchannel ATP sensitivity in human pancreatic β-cells and rat INS-1 cells

(2008) Guoxin Kang et al.   JOURNAL OF PHYSIOLOGY-LONDON

 -Arrestin-1 mediates glucagon-like peptide-1 signaling to insulin secretion in cultured pancreatic   cells

(2008) N. Sonoda et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Heterotrimeric G protein activation by G-protein-coupled receptors

(2007) William M. Oldham et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY