ArticleBiochemical pharmacology2016
Key interactions by conserved polar amino acids located at the transmembrane helical boundaries in Class B GPCRs modulate activation, effector specificity and biased signalling in the glucagon-like peptide-1 receptor.
Article in Biochemical pharmacology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
What it found
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Who cites it
24 citing papers in PubMed, 45 citations in OpenAlex.
- Citronellal Exerts Sedative-Like Effects and Augments Diazepam's Action in Swiss Mice, Possibly Through the GABAergic Pathway.Brain and behavior · 2025Article
- New Insights into the Structure and Function of Class B1 GPCRs.Endocrine reviews · 2023Article
- Mapping allosteric pathway in NIa-Pro using computational approach.Quantitative biology (Beijing, China) · 2023Article
- Anionic phospholipids control mechanisms of GPCR-G protein recognition.Nature communications · 2023Article
- Anionic Phospholipids Control Mechanisms of GPCR-G Protein Recognition.bioRxiv : the preprint server for biology · 2023Article
- Structural and functional diversity among agonist-bound states of the GLP-1 receptor.Nature chemical biology · 2022Article
- Evaluation of selected carotenoids of Lycopersicon esculentum variants as therapeutic targets for 'Alzheimer's disease: an in silico approach.BMC molecular and cell biology · 2021Article
- Concerted conformational dynamics and water movements in the ghrelin G protein-coupled receptor.eLife · 2021Article
- GLP-1 Val8: A Biased GLP-1R Agonist with Altered Binding Kinetics and Impaired Release of Pancreatic Hormones in Rats.ACS pharmacology & translational science · 2021Article
- Exploring Ligand Binding to Calcitonin Gene-Related Peptide Receptors.Frontiers in molecular biosciences · 2021Article
- Capturing Peptide-GPCR Interactions and Their Dynamics.Molecules (Basel, Switzerland) · 2020Review
- A combined activation mechanism for the glucagon receptor.Proceedings of the National Academy of Sciences of the United States of America · 2020Article
- Rational development of a high-affinity secretin receptor antagonist.Biochemical pharmacology · 2020Article
- Structure and Dynamics of Adrenomedullin Receptors AMACS pharmacology & translational science · 2020Article
- Structural Basis for Allosteric Modulation of Class B G Protein-Coupled Receptors.Annual review of pharmacology and toxicology · 2020Review
- A conserved molecular switch in Class F receptors regulates receptor activation and pathway selection.Nature communications · 2019Article
- Mechanisms of signalling and biased agonism in G protein-coupled receptors.Nature reviews. Molecular cell biology · 2018Review
- Hypoglycemic Effects of Intestinal Electrical Stimulation by Enhancing Nutrient-Stimulated Secretion of GLP-1 in Rats.Obesity surgery · 2018Article
- Two distinct domains of the glucagon-like peptide-1 receptor control peptide-mediated biased agonism.The Journal of biological chemistry · 2018Article
- Biased signalling: from simple switches to allosteric microprocessors.Nature reviews. Drug discovery · 2018Review
Corrections and comments
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Authors and funding
8 authors at 3 institutions in 3 countries.
Funding
Abstract
Class B GPCRs can activate multiple signalling effectors with the potential to exhibit biased agonism in response to ligand stimulation. Previously, we highlighted key TM domain polar amino acids that were crucial for the function of the GLP-1 receptor, a key therapeutic target for diabetes and obesity. Using a combination of mutagenesis, pharmacological characterisation, mathematical and computational molecular modelling, this study identifies additional highly conserved polar residues located towards the TM helical boundaries of Class B GPCRs that are important for GLP-1 receptor stability and/or controlling signalling specificity and biased agonism. This includes (i) three positively charged residues (R3.30
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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.