ArticleChemistryOpen2017
Potent Prearranged Positive Allosteric Modulators of the Glucagon-like Peptide-1 Receptor.
Article in ChemistryOpen, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed, 40 citations in OpenAlex.
- Prolonged signaling of backbone-modified glucagon-like peptide-Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Enhanced Endosomal Signaling and Desensitization of GLP-1R vs GIPR in Pancreatic Beta Cells.Endocrinology · 2023Article
- DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling.Angewandte Chemie (International ed. in English) · 2022Article
- Non-peptide agonists and positive allosteric modulators of glucagon-like peptide-1 receptors: Alternative approaches for treatment of Type 2 diabetes.British journal of pharmacology · 2022Review
- Discovery of small molecule positive allosteric modulators of the secretin receptor.Biochemical pharmacology · 2021Article
- Ligand-Specific Factors Influencing GLP-1 Receptor Post-Endocytic Trafficking and Degradation in Pancreatic Beta Cells.International journal of molecular sciences · 2020Article
- Mechanistic Insights into Light-Driven Allosteric Control of GPCR Biological Activity.ACS pharmacology & translational science · 2020Article
- Advances in therapeutic peptides targeting G protein-coupled receptors.Nature reviews. Drug discovery · 2020Review
- Perspective: Implications of Ligand-Receptor Binding Kinetics for Therapeutic Targeting of G Protein-Coupled Receptors.ACS pharmacology & translational science · 2020Review
- Agonist-induced membrane nanodomain clustering drives GLP-1 receptor responses in pancreatic beta cells.PLoS biology · 2019Article
- Optical tools for understanding the complexity of β-cell signalling and insulin release.Nature reviews. Endocrinology · 2018Review
- Targeting GLP-1 receptor trafficking to improve agonist efficacy.Nature communications · 2018Article
- Potent Prearranged Positive Allosteric Modulators of the Glucagon-like Peptide-1 Receptor.ChemistryOpen · 2017Article
Corrections and comments
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Authors and funding
6 authors at 5 institutions in 3 countries.
Funding
Abstract
Drugs that allosterically modulate G protein-coupled receptor (GPCR) activity display higher specificity and may improve disease treatment. However, the rational design of compounds that target the allosteric site is difficult, as conformations required for receptor activation are poorly understood. Guided by photopharmacology, a set of prearranged positive allosteric modulators (PAMs) with restricted degrees of freedom was designed and tested against the glucagon-like peptide-1 receptor (GLP-1R), a GPCR involved in glucose homeostasis. Compounds incorporating a
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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.