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A fluorescent approach for identifying P2X1 ligands.
Marc-David Ruepp, James A Brozik, Iwan JP de Esch, Richard W Farndale, Ruth D Murrell-Lagnado, Andrew J Thompson
Jun 15, 2015
Alexa-647 Fluorescent Fragment-based drug discovery Ligand binding Ligand gated ion channel NF449 P2X1 Pharmacology Adenosine Triphosphate Benzenesulfonates Binding Sites Carbocyanines Dose-Response Relationship Drug Fluorescence Gene Expression HEK293 Cells Humans Ligands Microscopy Confocal Purinergic P2X Receptor Agonists Purinergic P2X Receptor Antagonists Receptors Purinergic P2X1 Transfection Voltage-Sensitive Dye Imaging
A challenge finding P2X1 and P2X4 ligands.
Paul Beswick, Ben Wahab, Mark A Honey, Michael Paradowski, Ke Jiang, Martin Lochner, Ruth D Murrell-Lagnado, Andrew J Thompson
Jul 05, 2019
Identifying novel small-molecule P2X1 and P2X4 ligands with sub-type specificity and high-affinity remains a pharmacological challenge. Here we use computational methods, electrophysiology and fluorescent microplate assays to...
Agonist Antagonist Function Ion channel ligand Microplate P2X1 P2X4 screen Two-electrode voltage clamp Animals Biguanides Cells Cultured Computer Simulation Drug Discovery Humans Ligands Molecular Docking Simulation Oocytes Patch-Clamp Techniques Purinergic Agonists Purinergic Antagonists Receptors Purinergic P2X1 Receptors Purinergic P2X4 Structure-Activity Relationship Xenopus laevis