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- W2044181572 endingPage "360" @default.
- W2044181572 startingPage "350" @default.
- W2044181572 abstract "Pentameric ligand-gated ion channels (pLGICs) play a central role in intercellular communications in the nervous system by converting the binding of a chemical messenger—a neurotransmitter—into an ion flux through the postsynaptic membrane. They are oligomeric assemblies that provide prototypical examples of allosterically regulated integral membrane proteins. Here, we present an overview of the most recent advances on the signal transduction mechanism based on the X-ray structures of both prokaryotic and invertebrate eukaryotic pLGICs and atomistic Molecular Dynamics simulations. The present results suggest that ion gating involves a large structural reorganization of the molecule mediated by two distinct quaternary transitions, a global twisting and the blooming of the extracellular domain, which can be modulated by ligand binding at the topographically distinct orthosteric and allosteric sites. The emerging model of gating is consistent with a wealth of functional studies and will boost the development of novel pharmacological strategies." @default.
- W2044181572 created "2016-06-24" @default.
- W2044181572 creator A5014097984 @default.
- W2044181572 creator A5016364652 @default.
- W2044181572 creator A5054527529 @default.
- W2044181572 creator A5056074308 @default.
- W2044181572 date "2014-07-01" @default.
- W2044181572 modified "2023-10-09" @default.
- W2044181572 title "Allosteric regulation of pentameric ligand-gated ion channels: An emerging mechanistic perspective" @default.
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