Article: article from journal or magazin.
Ligand binding transmits conformational changes across the membrane-spanning region to the intracellular side of the 5-HT3 serotonin receptor.
Conformational changes of channel activation: Five enhanced green fluorescent protein (EGFP) molecules (green cylinders) were integrated into the intracellular part of the homopentameric ionotropic 5-HT3 receptor. This allowed the detection of extracellular binding of fluorescent ligands (?) to EGFP by FRET, and also enabled the quantification of agonist-induced conformational changes in the intracellular region of the receptor by homo-FRET between EGFPs. The approach opens novel ways for probing receptor activation and functional screening of therapeutic compounds.
Cell Line, Cell Membrane, Fluorescence Resonance Energy Transfer, Green Fluorescent Proteins, Humans, Ion Channels/metabolism, Ligands, Membrane Microdomains, Protein Binding, Protein Conformation, Receptors, Serotonin, 5-HT3/chemistry
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