Auto-inhibition at a ligand-gated ion channel: a cross-talk between orthosteric and allosteric sites
نویسندگان
چکیده
منابع مشابه
Common Internal Allosteric Network Links Anesthetic Binding Sites in a Pentameric Ligand-Gated Ion Channel
General anesthetics bind reversibly to ion channels, modifying their global conformational distributions, but the underlying atomic mechanisms are not completely known. We examine this issue by way of the model protein Gloeobacter violaceous ligand-gated ion channel (GLIC) using computational molecular dynamics, with a coarse-grained model to enhance sampling. We find that in flooding simulatio...
متن کاملAllosteric coupling in ligand-gated ion channels
What does " allosteric " mean? In the context of receptors, the word allosteric is now widely used. It is, perhaps, not helpful for clarity of thought that different authors often use it to mean somewhat different things (Colquhoun, 1998). At one extreme, the term " allosteric antagonist " can often be translated as " we have got an antagonist and we are not sure what it does, but it appears no...
متن کاملUn-gating and allosteric modulation of a pentameric ligand-gated ion channel captured by molecular dynamics
Pentameric ligand-gated ion channels (pLGICs) mediate intercellular communication at synapses through the opening of an ion pore in response to the binding of a neurotransmitter. Despite the increasing availability of high-resolution structures of pLGICs, a detailed understanding of the functional isomerization from closed to open (gating) and back is currently missing. Here, we provide the fir...
متن کاملSites of Anesthetic Inhibitory Action on a Cationic Ligand-Gated Ion Channel.
Pentameric ligand-gated ion channels have been identified as the principal target of general anesthetics (GA), whose molecular mechanism of action remains poorly understood. Bacterial homologs, such as the Gloeobacter violaceus receptor (GLIC), have been shown to be valid functional models of GA action. The GA bromoform inhibits GLIC at submillimolar concentration. We characterize bromoform bin...
متن کاملThe Ligand Gated Ion Channel Database
The ligand gated ion channels (LGICs) are ionotropic receptors to neurotransmitters. Their physiological effect is carried out by the opening of an ionic channel upon binding of a particular neurotransmitter. These LGICs constitute superfamilies of receptors formed by homologous subunits. A database has been developed to handle the growing wealth of cloned subunits. This database contains nucle...
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ژورنال
عنوان ژورنال: British Journal of Pharmacology
سال: 2014
ISSN: 0007-1188
DOI: 10.1111/bph.12896