ArticleScientific reports2016
Structural insight into antibody-mediated antagonism of the Glucagon-like peptide-1 Receptor.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 30 citations in OpenAlex.
- Review
- GLP- 1R status using validated monoclonal antibody in 689 cases of neuroendocrine neoplasm and its correlation with somatostatin receptor scintigraphy, insulin production, and histological grades.Virchows Archiv : an international journal of pathology · 2025Article
- Antibodies expand the scope of angiotensin receptor pharmacology.Nature chemical biology · 2024Article
- Rapid One-Step Capturing of Native, Cell-Free Synthesized and Membrane-Embedded GLP-1R.International journal of molecular sciences · 2023Article
- A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor.Journal of medicinal chemistry · 2022Article
- Scap structures highlight key role for rotation of intertwined luminal loops in cholesterol sensing.Cell · 2021Article
- Peptidyl and Non-Peptidyl Oral Glucagon-Like Peptide-1 Receptor Agonists.Endocrinology and metabolism (Seoul, Korea) · 2021Review
- MiR-27a-3p Targets GLP1R to Regulate Differentiation, Autophagy, and Release of Inflammatory Factors in Pre-OsteoblastsFrontiers in genetics · 2021Article
- The Interplay of Glucagon-Like Peptide-1 Receptor Trafficking and Signalling in Pancreatic Beta Cells.Frontiers in endocrinology · 2021Review
- Ligand-Specific Factors Influencing GLP-1 Receptor Post-Endocytic Trafficking and Degradation in Pancreatic Beta Cells.International journal of molecular sciences · 2020Article
- Synthetic nanobodies as angiotensin receptor blockers.Proceedings of the National Academy of Sciences of the United States of America · 2020Article
- Exendin-4 restores airway mucus homeostasis through the GLP1R-PKA-PPARγ-FOXA2-phosphatase signaling.Mucosal immunology · 2020Article
- Structural Basis for Allosteric Modulation of Class B G Protein-Coupled Receptors.Annual review of pharmacology and toxicology · 2020Review
- Structure-guided discovery of a single-domain antibody agonist against human apelin receptor.Science advances · 2020Article
- Development and characterisation of a novel glucagon like peptide-1 receptor antibody.Diabetologia · 2018Article
- Opportunities for therapeutic antibodies directed at G-protein-coupled receptors.Nature reviews. Drug discovery · 2017Review
- Rearrangement of a polar core provides a conserved mechanism for constitutive activation of class B G protein-coupled receptors.The Journal of biological chemistry · 2017Article
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Corrections and comments
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Authors and funding
12 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The Glucagon-like peptide-1 receptor (GLP-1R) is a member of the class B G protein-coupled receptor (GPCR) family and a well-established target for the treatment of type 2 diabetes. The N-terminal extracellular domain (ECD) of GLP-1R is important for GLP-1 binding and the crystal structure of the GLP-1/ECD complex was reported previously. The first structure of a class B GPCR transmembrane (TM) domain was solved recently, but the full length receptor structure is still not well understood. Here we describe the molecular details of antibody-mediated antagonism of the GLP-1R using both in vitro pharmacology and x-ray crystallography. We showed that the antibody Fab fragment (Fab 3F52) blocked the GLP-1 binding site of the ECD directly and thereby acts as a competitive antagonist of native GLP-1. Interestingly, Fab 3F52 also blocked a short peptide agonist believed to engage primarily the transmembrane and extracellular loop region of GLP-1R, whereas functionality of an allosteric small-molecule agonist was not inhibited. This study has implications for the structural understanding of the GLP-1R and related class B GPCRs, which is important for the development of new and improved therapeutics targeting these receptors.
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Registered trials
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.