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• W2000445778 endingPage "1855" @default.
• W2000445778 startingPage "1847" @default.
• W2000445778 abstract "The serotonin 5-HT(3) receptor (5-HT(3)R) is a member of the Cys-loop ligand-gated ion channel family. We used a combination of site-directed mutagenesis, homology modeling, and ligand-docking simulations to analyze antagonist-receptor interactions. Mutation of E236, which is near loop C of the binding site, to aspartate prevents expression of the receptor on the cell surface, and no specific ligand binding can be detected. On the other hand, mutation to glutamine, asparagine, or alanine produces receptors that are expressed on the cell surface, but decreases receptor affinity for the competitive antagonist d-tubocurarine (dTC) 5-35-fold. The results of a double-mutant cycle analysis employing a panel of dTC analogs to identify specific points of interactions between the dTC analogs and E236 are consistent with E236 making a direct physical interaction with the 12 -OH of dTC. dTC is a rigid molecule of known three-dimensional structure. Together with previous studies linking other regions of dTC to specific residues in the binding site, these data allow us to define the relative spatial arrangement of three different residues in the ligand-binding site: R92 (loop D), N128 (loop A), and E236 (near loop C). Molecular modeling employing these distance constraints followed by molecular-dynamics simulations produced a dTC/receptor complex consistent with the experimental data. The use of the rigid ligands as molecular rulers in conjunction with double-mutant cycle analysis provides a means of mapping the relative positions of various residues in the ligand-binding site of any ligand-receptor complex, and thus is a useful tool for delineating the architecture of the binding site." @default.
• W2000445778 created "2016-06-24" @default.
• W2000445778 creator A5038508476 @default.
• W2000445778 creator A5052562213 @default.
• W2000445778 creator A5058605663 @default.
• W2000445778 creator A5073091304 @default.
• W2000445778 date "2010-05-01" @default.
• W2000445778 modified "2023-09-23" @default.
• W2000445778 title "Mapping Spatial Relationships between Residues in the Ligand-Binding Domain of the 5-Ht3 Receptor Using a Molecular Ruler" @default.
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• W2000445778 doi "https://doi.org/10.1016/j.bpj.2010.01.034" @default.
• W2000445778 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/2862198" @default.
• W2000445778 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/20441748" @default.
• W2000445778 hasPublicationYear "2010" @default.
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