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• W2793207668 abstract "General anesthetics are thought to allosterically bind and potentiate the inhibitory currents of the GABAA receptor through drug-specific binding sites. The physiologically relevant isoform of the GABAA receptor is a transmembrane ligand-gated ion channel consisting of five subunits (γ-α-β-α-β linkage) symmetrically arranged around a central chloride-conducting pore. Although the exact molecular structure of this heteropentameric GABAA receptor remains unknown, molecular modeling has allowed significant advancements in understanding anesthetic binding and action. Using the open-channel conformations of the homologous glycine and glutamate-gated chloride receptors as templates, a homology model of the GABAA receptor was constructed using the Discovery Studio computational chemistry software suite. Consensus structural alignment of the homology templates allowed for the construction of a three-dimensional heteropentameric GABAA receptor model with (γ2-β3-α1-β3-α1) subunit linkage. An anesthetic binding site was identified within the transmembrane α/β intersubunit space by the convergence of three residues shown to be essential for anesthetic activity in previous studies with mutant mice (β3-N265, β3-M286, α1-L232). Propofol derivatives docked into this binding site showed log-linear correlation with experimentally derived GABAA receptor potentiation (EC50) values, suggesting this binding site may be important for receptor activation. The receptor-based pharmacophore was analyzed with surface maps displaying the predominant anesthetic-protein interactions, revealing an amphiphilic binding cavity incorporating the three residues involved in anesthetic modulation. Quantum mechanics calculations of the bonding patterns found in complementary high-resolution receptor systems further elucidated the complex nature of anesthetic-protein interactions." @default.
• W2793207668 created "2018-03-29" @default.
• W2793207668 creator A5043389413 @default.
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• W2793207668 date "2018-01-01" @default.
• W2793207668 modified "2023-10-16" @default.
• W2793207668 title "Insights Into Receptor-Based Anesthetic Pharmacophores and Anesthetic–Protein Interactions" @default.
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• W2793207668 doi "https://doi.org/10.1016/bs.mie.2018.01.004" @default.
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