Ligand binding transmits conformational changes across the membrane-spanning region to the intracellular side of the 5-HT3 serotonin receptor.
Détails
ID Serval
serval:BIB_140913F3837F
Type
Article: article d'un périodique ou d'un magazine.
Collection
Publications
Institution
Titre
Ligand binding transmits conformational changes across the membrane-spanning region to the intracellular side of the 5-HT3 serotonin receptor.
Périodique
ChemBioChem
ISSN
1439-4227[print], 1439-4227[linking]
Statut éditorial
Publié
Date de publication
2005
Volume
6
Numéro
12
Pages
2180-2185
Langue
anglais
Résumé
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.
Mots-clé
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
Pubmed
Web of science
Création de la notice
24/01/2008 13:45
Dernière modification de la notice
20/08/2019 13:42
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