ArticleProceedings of the National Academy of Sciences of the United States of America2007
Small-molecule agonists for the glucagon-like peptide 1 receptor.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 105 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
105 citing papers in PubMed, 225 citations in OpenAlex.
- An experimental medicine protocol for exploring the haemodynamic effects of dual agonism at the glucagon-like peptide-1 and glucagon receptor in healthy subjects.British journal of clinical pharmacology · 2026Trial
- Exenatide and glucagon co-infusion increases myocardial glucose uptake and improves markers of diastolic dysfunction in adults with type 2 diabetes.Scientific reports · 2025Trial
- Igniting antitumour immunity with cancer cell pyroptosis.Nature reviews. Cancer · 2026Review
- The evolving landscape of obesity pharmacotherapy.Nature reviews. Drug discovery · 2026Review
- Identification and Characterization of a Phenyl(trifluoro-methyl)-pyrimidine Positive Allosteric Modulator of the Secretin Receptor.Membranes · 2026Article
- A rationally designed 18-amino acid peptide with potential as GLP-1 receptor agonist.Frontiers in pharmacology · 2026Article
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- Molecular docking of danuglipron uncovers potential crossovers between GLP-1R and the endocannabinoid system.microPublication biology · 2025Article
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- QnAs with Svetlana Mojsov, Joel Habener, and Lotte Bjerre Knudsen: Winners of the 2024 Lasker~DeBakey Clinical Medical Research Award.Proceedings of the National Academy of Sciences of the United States of America · 2024Article
- Prolonged Activation of the GLP-1 Receptor via Covalent Capture.ACS chemical biology · 2024Article
- Comparative Analysis of Orthosteric and Allosteric GLP-1R Agonists' Effects on Insulin Secretion from Healthy, Diabetic, and Recovered INS-1E Pancreatic Beta Cells.International journal of molecular sciences · 2024Article
- Cryo-electron microscopy for GPCR research and drug discovery in endocrinology and metabolism.Nature reviews. Endocrinology · 2024Review
- G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery.Signal transduction and targeted therapy · 2024Review
- Human GLP1R variants affecting GLP1R cell surface expression are associated with impaired glucose control and increased adiposity.Nature metabolism · 2023Article
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- Affinity selection of double-click triazole libraries for rapid discovery of allosteric modulators for GLP-1 receptor.Proceedings of the National Academy of Sciences of the United States of America · 2023Article
- A physiologic increase in brain glucagon action alters the hepatic gluconeogenic/glycogenolytic ratio but not glucagon's overall effect on glucose production.American journal of physiology. Endocrinology and metabolism · 2023Article
- GLP-1R Signaling and Functional Molecules in Incretin Therapy.Molecules (Basel, Switzerland) · 2023Review
- Improved Split TEV GPCR β-arrestin-2 Recruitment Assays via Systematic Analysis of Signal Peptide and β-arrestin Binding Motif Variants.Biosensors · 2022Article
45 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
22 authors at 5 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The peptide hormone glucagon-like peptide (GLP)-1 has important actions resulting in glucose lowering along with weight loss in patients with type 2 diabetes. As a peptide hormone, GLP-1 has to be administered by injection. Only a few small-molecule agonists to peptide hormone receptors have been described and none in the B family of the G protein coupled receptors to which the GLP-1 receptor belongs. We have discovered a series of small molecules known as ago-allosteric modulators selective for the human GLP-1 receptor. These compounds act as both allosteric activators of the receptor and independent agonists. Potency of GLP-1 was not changed by the allosteric agonists, but affinity of GLP-1 for the receptor was increased. The most potent compound identified stimulates glucose-dependent insulin release from normal mouse islets but, importantly, not from GLP-1 receptor knockout mice. Also, the compound stimulates insulin release from perfused rat pancreas in a manner additive with GLP-1 itself. These compounds may lead to the identification or design of orally active GLP-1 agonists.
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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.