ArticleMolecular pharmacology2021
Acylation of the Incretin Peptide Exendin-4 Directly Impacts Glucagon-Like Peptide-1 Receptor Signaling and Trafficking.
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Article in Molecular pharmacology, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 36 citations in OpenAlex.
- Pharmacokinetics and Food Effect of HDM1002, a Novel Oral Small-Molecule GLP-1 Receptor Agonist, in Healthy Chinese Volunteers: A Bioequivalence Study.Diabetes, obesity & metabolism · 2026Trial
- Identification of PfSR1-MT as melatonin-responsive GPCR-like candidate from the human malaria parasiteCurrent research in microbial sciences · 2026Article
- Unimolecular GLP-1/Apelin Hybrid Peptides Cause Prominent Appetite Suppression, as Well as Enhancing Insulin Secretion, Beta-Cell Survival and Glycaemic Regulation.Diabetes, obesity & metabolism · 2026Article
- Modelling G protein-biased agonism using GLP-1 receptor C-terminal mutations.Molecular metabolism · 2026Article
- In vivo functional profiling and structural characterization of the humanScience advances · 2026Article
- Human class B1 GPCR modulation by plasma membrane lipids.Communications biology · 2026Article
- Review
- Prolonging parathyroid hormone analog action in vitro and in vivo through peptide lipidation.Nature communications · 2025Article
- Molecular mapping and functional validation of GLP-1R cholesterol binding sites in pancreatic beta cells.eLife · 2025Article
- Prolonged signaling of backbone-modified glucagon-like peptide-Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- 2FA-Platform Generates Dual Fatty Acid-Conjugated GLP-1 Receptor Agonist TE-8105 with Enhanced Diabetes, Obesity, and NASH Efficacy Compared to Semaglutide.Journal of medicinal chemistry · 2025Article
- A Comprehensive Review on the Pharmacokinetics and Drug-Drug Interactions of Approved GLP-1 Receptor Agonists and a Dual GLP-1/GIP Receptor Agonist.Drug design, development and therapy · 2025Review
- Glucagon-like peptide-1 receptor: mechanisms and advances in therapy.Signal transduction and targeted therapy · 2024 · on this mapReview
- Lipid regulation of the glucagon receptor family.The Journal of endocrinology · 2024Review
- Brain access of incretins and incretin receptor agonists to their central targets relevant for appetite suppression and weight loss.American journal of physiology. Endocrinology and metabolism · 2024Review
- New Insights into the Structure and Function of Class B1 GPCRs.Endocrine reviews · 2023Article
- Divergent acute versus prolonged pharmacological GLP-1R responses in adult β cell-specific β-arrestin 2 knockout mice.Science advances · 2023Article
- Measuring Protein-Protein Interactions of Melatonin Receptors by Bioluminescence Resonance Energy Transfer (BRET).Methods in molecular biology (Clifton, N.J.) · 2022Article
- Reagents and models for detecting endogenous GLP1R and GIPR.EBioMedicine · 2021Review
- Evaluation of efficacy- versus affinity-driven agonism with biased GLP-1R ligands P5 and exendin-F1.Biochemical pharmacology · 2021Article
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Authors and funding
15 authors at 9 institutions in 4 countries.
Maria LuceySection of Endocrinology and Investigative Medicine (M.L., T.A., A.M., J.M., S.R.B., B.J.) and Section of Cell Biology and Functional Genomics (Y.W., A.T.), Department of Metabolism, Digestion and Reproduction, and Department of Chemical Engineering (Y.E.), Imperial College London, London, United Kingdom; Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom (J.G., S.J.B.); Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, United Kingdom (J.G., D.J.H., S.J.B.); Université de Paris, Institut Cochin, INSERM, CNRS, Paris, France (A.O., R.J.); Department of Anatomy, Kyorin University Faculty of Medicine, Tokyo, Japan (A.O.); Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany (J.B.); Institute of Metabolism and Systems Research (IMSR), University of Birmingham, Birmingham, United Kingdom (D.J.H.); and Centre for Endocrinology, Diabetes and Metabolism, Birmingham Health Partners, Birmingham, United Kingdom (D.J.H.).
Tanyel AshikSection of Endocrinology and Investigative Medicine (M.L., T.A., A.M., J.M., S.R.B., B.J.) and Section of Cell Biology and Functional Genomics (Y.W., A.T.), Department of Metabolism, Digestion and Reproduction, and Department of Chemical Engineering (Y.E.), Imperial College London, London, United Kingdom; Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom (J.G., S.J.B.); Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, United Kingdom (J.G., D.J.H., S.J.B.); Université de Paris, Institut Cochin, INSERM, CNRS, Paris, France (A.O., R.J.); Department of Anatomy, Kyorin University Faculty of Medicine, Tokyo, Japan (A.O.); Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany (J.B.); Institute of Metabolism and Systems Research (IMSR), University of Birmingham, Birmingham, United Kingdom (D.J.H.); and Centre for Endocrinology, Diabetes and Metabolism, Birmingham Health Partners, Birmingham, United Kingdom (D.J.H.).
Amaara MarzookSection of Endocrinology and Investigative Medicine (M.L., T.A., A.M., J.M., S.R.B., B.J.) and Section of Cell Biology and Functional Genomics (Y.W., A.T.), Department of Metabolism, Digestion and Reproduction, and Department of Chemical Engineering (Y.E.), Imperial College London, London, United Kingdom; Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom (J.G., S.J.B.); Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, United Kingdom (J.G., D.J.H., S.J.B.); Université de Paris, Institut Cochin, INSERM, CNRS, Paris, France (A.O., R.J.); Department of Anatomy, Kyorin University Faculty of Medicine, Tokyo, Japan (A.O.); Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany (J.B.); Institute of Metabolism and Systems Research (IMSR), University of Birmingham, Birmingham, United Kingdom (D.J.H.); and Centre for Endocrinology, Diabetes and Metabolism, Birmingham Health Partners, Birmingham, United Kingdom (D.J.H.).
Yifan WangSection of Endocrinology and Investigative Medicine (M.L., T.A., A.M., J.M., S.R.B., B.J.) and Section of Cell Biology and Functional Genomics (Y.W., A.T.), Department of Metabolism, Digestion and Reproduction, and Department of Chemical Engineering (Y.E.), Imperial College London, London, United Kingdom; Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom (J.G., S.J.B.); Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, United Kingdom (J.G., D.J.H., S.J.B.); Université de Paris, Institut Cochin, INSERM, CNRS, Paris, France (A.O., R.J.); Department of Anatomy, Kyorin University Faculty of Medicine, Tokyo, Japan (A.O.); Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany (J.B.); Institute of Metabolism and Systems Research (IMSR), University of Birmingham, Birmingham, United Kingdom (D.J.H.); and Centre for Endocrinology, Diabetes and Metabolism, Birmingham Health Partners, Birmingham, United Kingdom (D.J.H.).
Joëlle GouldingSection of Endocrinology and Investigative Medicine (M.L., T.A., A.M., J.M., S.R.B., B.J.) and Section of Cell Biology and Functional Genomics (Y.W., A.T.), Department of Metabolism, Digestion and Reproduction, and Department of Chemical Engineering (Y.E.), Imperial College London, London, United Kingdom; Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom (J.G., S.J.B.); Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, United Kingdom (J.G., D.J.H., S.J.B.); Université de Paris, Institut Cochin, INSERM, CNRS, Paris, France (A.O., R.J.); Department of Anatomy, Kyorin University Faculty of Medicine, Tokyo, Japan (A.O.); Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany (J.B.); Institute of Metabolism and Systems Research (IMSR), University of Birmingham, Birmingham, United Kingdom (D.J.H.); and Centre for Endocrinology, Diabetes and Metabolism, Birmingham Health Partners, Birmingham, United Kingdom (D.J.H.).
Atsuro OishiSection of Endocrinology and Investigative Medicine (M.L., T.A., A.M., J.M., S.R.B., B.J.) and Section of Cell Biology and Functional Genomics (Y.W., A.T.), Department of Metabolism, Digestion and Reproduction, and Department of Chemical Engineering (Y.E.), Imperial College London, London, United Kingdom; Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom (J.G., S.J.B.); Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, United Kingdom (J.G., D.J.H., S.J.B.); Université de Paris, Institut Cochin, INSERM, CNRS, Paris, France (A.O., R.J.); Department of Anatomy, Kyorin University Faculty of Medicine, Tokyo, Japan (A.O.); Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany (J.B.); Institute of Metabolism and Systems Research (IMSR), University of Birmingham, Birmingham, United Kingdom (D.J.H.); and Centre for Endocrinology, Diabetes and Metabolism, Birmingham Health Partners, Birmingham, United Kingdom (D.J.H.).
Johannes BroichhagenSection of Endocrinology and Investigative Medicine (M.L., T.A., A.M., J.M., S.R.B., B.J.) and Section of Cell Biology and Functional Genomics (Y.W., A.T.), Department of Metabolism, Digestion and Reproduction, and Department of Chemical Engineering (Y.E.), Imperial College London, London, United Kingdom; Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom (J.G., S.J.B.); Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, United Kingdom (J.G., D.J.H., S.J.B.); Université de Paris, Institut Cochin, INSERM, CNRS, Paris, France (A.O., R.J.); Department of Anatomy, Kyorin University Faculty of Medicine, Tokyo, Japan (A.O.); Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany (J.B.); Institute of Metabolism and Systems Research (IMSR), University of Birmingham, Birmingham, United Kingdom (D.J.H.); and Centre for Endocrinology, Diabetes and Metabolism, Birmingham Health Partners, Birmingham, United Kingdom (D.J.H.).
David J HodsonSection of Endocrinology and Investigative Medicine (M.L., T.A., A.M., J.M., S.R.B., B.J.) and Section of Cell Biology and Functional Genomics (Y.W., A.T.), Department of Metabolism, Digestion and Reproduction, and Department of Chemical Engineering (Y.E.), Imperial College London, London, United Kingdom; Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom (J.G., S.J.B.); Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, United Kingdom (J.G., D.J.H., S.J.B.); Université de Paris, Institut Cochin, INSERM, CNRS, Paris, France (A.O., R.J.); Department of Anatomy, Kyorin University Faculty of Medicine, Tokyo, Japan (A.O.); Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany (J.B.); Institute of Metabolism and Systems Research (IMSR), University of Birmingham, Birmingham, United Kingdom (D.J.H.); and Centre for Endocrinology, Diabetes and Metabolism, Birmingham Health Partners, Birmingham, United Kingdom (D.J.H.).
James MinnionSection of Endocrinology and Investigative Medicine (M.L., T.A., A.M., J.M., S.R.B., B.J.) and Section of Cell Biology and Functional Genomics (Y.W., A.T.), Department of Metabolism, Digestion and Reproduction, and Department of Chemical Engineering (Y.E.), Imperial College London, London, United Kingdom; Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom (J.G., S.J.B.); Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, United Kingdom (J.G., D.J.H., S.J.B.); Université de Paris, Institut Cochin, INSERM, CNRS, Paris, France (A.O., R.J.); Department of Anatomy, Kyorin University Faculty of Medicine, Tokyo, Japan (A.O.); Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany (J.B.); Institute of Metabolism and Systems Research (IMSR), University of Birmingham, Birmingham, United Kingdom (D.J.H.); and Centre for Endocrinology, Diabetes and Metabolism, Birmingham Health Partners, Birmingham, United Kingdom (D.J.H.).
Yuval ElaniSection of Endocrinology and Investigative Medicine (M.L., T.A., A.M., J.M., S.R.B., B.J.) and Section of Cell Biology and Functional Genomics (Y.W., A.T.), Department of Metabolism, Digestion and Reproduction, and Department of Chemical Engineering (Y.E.), Imperial College London, London, United Kingdom; Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom (J.G., S.J.B.); Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, United Kingdom (J.G., D.J.H., S.J.B.); Université de Paris, Institut Cochin, INSERM, CNRS, Paris, France (A.O., R.J.); Department of Anatomy, Kyorin University Faculty of Medicine, Tokyo, Japan (A.O.); Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany (J.B.); Institute of Metabolism and Systems Research (IMSR), University of Birmingham, Birmingham, United Kingdom (D.J.H.); and Centre for Endocrinology, Diabetes and Metabolism, Birmingham Health Partners, Birmingham, United Kingdom (D.J.H.).
Ralf JockersSection of Endocrinology and Investigative Medicine (M.L., T.A., A.M., J.M., S.R.B., B.J.) and Section of Cell Biology and Functional Genomics (Y.W., A.T.), Department of Metabolism, Digestion and Reproduction, and Department of Chemical Engineering (Y.E.), Imperial College London, London, United Kingdom; Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom (J.G., S.J.B.); Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, United Kingdom (J.G., D.J.H., S.J.B.); Université de Paris, Institut Cochin, INSERM, CNRS, Paris, France (A.O., R.J.); Department of Anatomy, Kyorin University Faculty of Medicine, Tokyo, Japan (A.O.); Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany (J.B.); Institute of Metabolism and Systems Research (IMSR), University of Birmingham, Birmingham, United Kingdom (D.J.H.); and Centre for Endocrinology, Diabetes and Metabolism, Birmingham Health Partners, Birmingham, United Kingdom (D.J.H.).
Stephen J BriddonSection of Endocrinology and Investigative Medicine (M.L., T.A., A.M., J.M., S.R.B., B.J.) and Section of Cell Biology and Functional Genomics (Y.W., A.T.), Department of Metabolism, Digestion and Reproduction, and Department of Chemical Engineering (Y.E.), Imperial College London, London, United Kingdom; Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom (J.G., S.J.B.); Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, United Kingdom (J.G., D.J.H., S.J.B.); Université de Paris, Institut Cochin, INSERM, CNRS, Paris, France (A.O., R.J.); Department of Anatomy, Kyorin University Faculty of Medicine, Tokyo, Japan (A.O.); Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany (J.B.); Institute of Metabolism and Systems Research (IMSR), University of Birmingham, Birmingham, United Kingdom (D.J.H.); and Centre for Endocrinology, Diabetes and Metabolism, Birmingham Health Partners, Birmingham, United Kingdom (D.J.H.).
Stephen R BloomSection of Endocrinology and Investigative Medicine (M.L., T.A., A.M., J.M., S.R.B., B.J.) and Section of Cell Biology and Functional Genomics (Y.W., A.T.), Department of Metabolism, Digestion and Reproduction, and Department of Chemical Engineering (Y.E.), Imperial College London, London, United Kingdom; Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom (J.G., S.J.B.); Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, United Kingdom (J.G., D.J.H., S.J.B.); Université de Paris, Institut Cochin, INSERM, CNRS, Paris, France (A.O., R.J.); Department of Anatomy, Kyorin University Faculty of Medicine, Tokyo, Japan (A.O.); Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany (J.B.); Institute of Metabolism and Systems Research (IMSR), University of Birmingham, Birmingham, United Kingdom (D.J.H.); and Centre for Endocrinology, Diabetes and Metabolism, Birmingham Health Partners, Birmingham, United Kingdom (D.J.H.).
Alejandra TomasSection of Endocrinology and Investigative Medicine (M.L., T.A., A.M., J.M., S.R.B., B.J.) and Section of Cell Biology and Functional Genomics (Y.W., A.T.), Department of Metabolism, Digestion and Reproduction, and Department of Chemical Engineering (Y.E.), Imperial College London, London, United Kingdom; Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom (J.G., S.J.B.); Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, United Kingdom (J.G., D.J.H., S.J.B.); Université de Paris, Institut Cochin, INSERM, CNRS, Paris, France (A.O., R.J.); Department of Anatomy, Kyorin University Faculty of Medicine, Tokyo, Japan (A.O.); Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany (J.B.); Institute of Metabolism and Systems Research (IMSR), University of Birmingham, Birmingham, United Kingdom (D.J.H.); and Centre for Endocrinology, Diabetes and Metabolism, Birmingham Health Partners, Birmingham, United Kingdom (D.J.H.) ben.jones@imperial.ac.uk a.tomas-catala@imperial.ac.uk.
Ben JonesSection of Endocrinology and Investigative Medicine (M.L., T.A., A.M., J.M., S.R.B., B.J.) and Section of Cell Biology and Functional Genomics (Y.W., A.T.), Department of Metabolism, Digestion and Reproduction, and Department of Chemical Engineering (Y.E.), Imperial College London, London, United Kingdom; Division of Physiology, Pharmacology and Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom (J.G., S.J.B.); Centre of Membrane Proteins and Receptors (COMPARE), University of Birmingham and University of Nottingham, Midlands, United Kingdom (J.G., D.J.H., S.J.B.); Université de Paris, Institut Cochin, INSERM, CNRS, Paris, France (A.O., R.J.); Department of Anatomy, Kyorin University Faculty of Medicine, Tokyo, Japan (A.O.); Leibniz-Forschungsinstitut für Molekulare Pharmakologie, Berlin, Germany (J.B.); Institute of Metabolism and Systems Research (IMSR), University of Birmingham, Birmingham, United Kingdom (D.J.H.); and Centre for Endocrinology, Diabetes and Metabolism, Birmingham Health Partners, Birmingham, United Kingdom (D.J.H.) ben.jones@imperial.ac.uk a.tomas-catala@imperial.ac.uk.
Kyorin University · JPLeibniz-Forschungsinstitut für Molekulare Pharmakologie · DEUniversité Paris Cité · FRUniversity of Nottingham · GBCentre National de la Recherche Scientifique · FRImperial College London · GBInserm · FRInstitut Cochin · FRUniversity of Birmingham · GB
Funding
Biotechnology and Biological Sciences Research CouncilDepartment of HealthMedical Research Council MR/K023667/1Medical Research Council MR/N00275X/1Medical Research Council MR/N020081/1Medical Research Council MR/R010676/1Medical Research Council MR/S025618/1Medical Research Council MR/S031537/1
Abstract
The glucagon-like peptide-1 receptor (GLP-1R) is a class B G protein-coupled receptor and mainstay therapeutic target for the treatment of type 2 diabetes and obesity. Recent reports have highlighted how biased agonism at the GLP-1R affects sustained glucose-stimulated insulin secretion through avoidance of desensitization and downregulation. A number of GLP-1R agonists (GLP-1RAs) feature a fatty acid moiety to prolong their pharmacokinetics via increased albumin binding, but the potential for these chemical changes to influence GLP-1R function has rarely been investigated beyond potency assessments for cAMP. Here, we directly compare the prototypical GLP-1RA exendin-4 with its C-terminally acylated analog, exendin-4-C16. We examine relative propensities of each ligand to recruit and activate G proteins and
Indexed as
AcylationAnimalsExenatideGlucagon-Like Peptide-1 ReceptorHEK293 CellsHumansIncretinsInsulin SecretionMaleMiceMice, Inbred C57BLProtein TransportSignal TransductionExenatideGLP1R protein, humanGlucagon-Like Peptide-1 ReceptorIncretins
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