Ligand binding transmits conformational changes across the membrane-spanning region to the intracellular side of the 5-HT3 serotonin receptor.

Details

Serval ID
serval:BIB_140913F3837F
Type
Article: article from journal or magazin.
Collection
Publications
Institution
Title
Ligand binding transmits conformational changes across the membrane-spanning region to the intracellular side of the 5-HT3 serotonin receptor.
Journal
ChemBioChem
Author(s)
Ilegems E., Pick H., Deluz C., Kellenberger S., Vogel H.
ISSN
1439-4227[print], 1439-4227[linking]
Publication state
Published
Issued date
2005
Volume
6
Number
12
Pages
2180-2185
Language
english
Abstract
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.
Keywords
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
Create date
24/01/2008 12:45
Last modification date
20/08/2019 12:42
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