ArticleChemistry & biology2012
Fragment screening at adenosine-A(3) receptors in living cells using a fluorescence-based binding assay.
Article in Chemistry & biology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 41 papers.
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Who cites it
41 citing papers in PubMed.
- Characterising C-X-C Chemokine Receptor 4 Dynamics in the Cell Membrane Using Fluorescence Fluctuation Spectroscopy.Biomolecules · 2026Article
- Dual blockade of adenosine AFrontiers in immunology · 2026Article
- Molecular basis of ligand binding and receptor activation at the human ANature communications · 2025Article
- Ligand-Directed Labeling of the Adenosine AJournal of medicinal chemistry · 2024Article
- Highly Selective Drug-Derived Fluorescent Probes for the Cannabinoid Receptor Type 1 (CBJournal of medicinal chemistry · 2024Article
- Target-based drug discovery: Applications of fluorescence techniques in high throughput and fragment-based screening.Heliyon · 2024Review
- Article
- Development and Characterization of Potent Succinate Receptor Fluorescent Tracers.Journal of medicinal chemistry · 2023Article
- New paradigms in purinergic receptor ligand discovery.Neuropharmacology · 2023Review
- Bioorthogonal Tethering Enhances Drug Fragment Affinity for G Protein-Coupled Receptors in Live Cells.Journal of the American Chemical Society · 2023Article
- Expanding the apelin receptor pharmacological toolbox using novel fluorescent ligands.Frontiers in endocrinology · 2023Article
- High-throughput screening strategies for space-based radiation countermeasure discovery.Life sciences in space research · 2022Review
- Selective activation of Gαob by an adenosine ANature communications · 2022Article
- Discovery of a High Affinity Adenosine AACS medicinal chemistry letters · 2022Article
- Live-cell microscopy or fluorescence anisotropy with budded baculoviruses-which way to go with measuring ligand binding to MOpen biology · 2022Article
- Structure-based identification of dual ligands at the AJournal of cheminformatics · 2021Article
- Molecular probes for the human adenosine receptors.Purinergic signalling · 2021Review
- Pharmacological characterisation of novel adenosine AScientific reports · 2020Article
- Fluorescent ligands: Bringing light to emerging GPCR paradigms.British journal of pharmacology · 2020Review
- Chemical Probes for the Adenosine Receptors.Pharmaceuticals (Basel, Switzerland) · 2019Review
Corrections and comments
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Authors and funding
6 authors.
Funding
Abstract
G protein-coupled receptors (GPCRs) comprise the largest family of transmembrane proteins. For GPCR drug discovery, it is important that ligand affinity is determined in the correct cellular environment and preferably using an unmodified receptor. We developed a live cell high-content screening assay that uses a fluorescent antagonist, CA200645, to determine binding affinity constants of competing ligands at human adenosine-A(1) and -A(3) receptors. This method was validated as a tool to screen a library of low molecular weight fragments, and identified a hit with submicromolar binding affinity (K(D)). This fragment was structurally unrelated to substructures of known adenosine receptor antagonists and was optimized to show selectivity for the adenosine-A(3) receptor. This technology represents a significant advance that will allow the determination of ligand and fragment affinities at receptors in their native membrane environment.
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Registered trials
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