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- W2069400364 abstract "Cys-loop receptors are a superfamily of ligand gated ion channels comprising such receptors as acetylcholine, serotonin, Glycine and GABA. Despite the low level of sequence conservation all these receptors are thought to share common structural characteristics. Numerous experiments describe in detail the pore channel and the extracellular domain. However due to the low sequence conservation between members of Cys-loop family, and the lack of any high resolution structures of these receptors in the trans-membrane domain (TMD), little information is available concerning the potential allosteric binding site. This potentiating binding site is of extreme importance for a pharmacological perspective, as it is the target of anesthetic an alcohol molecules. Recently the crystal structure of the open form of Gloeobacter violaceus pentameric ligand-gated ion channel (GLIC) has been solved [1]. As Glycine receptors (GlyR) are the closest receptors in terms of sequence, to GLIC, we decided to create a homology model of the human homomeric alpha-1 GlyR. Furthermore we chose the well-known ethanol molecule as a ligand target for studying the potentiating effect of such molecules on Cys-loop receptors [2]. In total we present 2 microseconds of molecular dynamics simulations, the longest simulation ever presented for Cys-loop receptors. Our simulations show a spontaneous binding of ethanol in cavities of the TMD. These cavities are located between subunits of GlyR TMD, and involve several residues previously identified by mutations as crucial for the potentiating effect of GlyR by ethanol. We also show that ethanol is stabilizing the open form of the GlyR, which could explain the effect of allosteric ligand on Cys-loop receptors. [1] Bocquet, N, et al. Nature (2009): (457)111-114. [2] Harris, RA, Trudell, JR and Mihic, SJ. Sci Signal. (2008): 1(28):re7." @default.
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- W2069400364 date "2010-01-01" @default.
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- W2069400364 title "Microsecond Simulations Show that Ethanol Binds between Subunits and Stabilizes the Open Form of a Glycine Receptor Model" @default.
- W2069400364 doi "https://doi.org/10.1016/j.bpj.2009.12.3865" @default.
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