title: Activation and modulation of ligand-gated ion channels.
abstract: Ligand-gated ionic channels are integral membrane proteins that enable rapid and selective ion fluxes across biological membranes. In excitable cells, their role is crucial for generation and propagation of electrical signals. This survey describes recent results from studies performed in the Department of Cellular Neurophysiology, Institute of Physiology ASCR, aimed at exploring the conformational dynamics of the acetylcholine, glutamate and vanilloid receptors during their activation, inactivation and desensitization. Distinct families of ion channels were selected to illustrate a rich complexity of the functional states and conformational transitions these proteins undergo. Particular attention is focused on structure-function studies and allosteric modulation of their activity. Comprehension of the fundamental principles of mechanisms involved in the operation of ligand-gated ion channels at the cellular and molecular level is an essential prerequisite for gaining an insight into the pathogenesis of many psychiatric and neurological disorders and for efficient development of novel specifically targeted drugs.
authors.affiliation: Departent of Cellular Neurophysiology, Institute of Physiology, Academy of Sciences of the Czech Republic, Prague, Czech Republic.
authors.forename: J
authors.initials: J
authors.lastname: Krůsek
authors.forename: I
authors.initials: I
authors.lastname: Dittert
authors.forename: T
authors.initials: T
authors.lastname: Hendrych
authors.forename: P
authors.initials: P
authors.lastname: Hník
authors.forename: M
authors.initials: M
authors.lastname: Horák
authors.forename: M
authors.initials: M
authors.lastname: Petrovic
authors.forename: M
authors.initials: M
authors.lastname: Sedlácek
authors.forename: K
authors.initials: K
authors.lastname: Susánková
authors.forename: L
authors.initials: L
authors.lastname: Svobodová
authors.forename: K
authors.initials: K
authors.lastname: Tousová
authors.forename: E
authors.initials: E
authors.lastname: Ujec
authors.forename: V
authors.initials: V
authors.lastname: Vlachová
authors.forename: L
authors.initials: L
authors.lastname: Vyklický
authors.forename: F
authors.initials: F
authors.lastname: Vyskocil
authors.forename: L
authors.initials: L
authors.lastname: Vyklický
mesh_terms: D000494:Allosteric Regulation; D000595:Amino Acid Sequence; D000818:Animals; D004594:Electrophysiology; D006801:Humans; D015640:Ion Channel Gating / Q000502:physiology*; D007473:Ion Channels / Q000502:physiology*; D008024:Ligands; D008969:Molecular Sequence Data; D011956:Receptors, Cell Surface / Q000378:metabolism*; D011950:Receptors, Cholinergic / Q000378:metabolism; D011955:Receptors, Drug / Q000378:metabolism; D017470:Receptors, Glutamate / Q000378:metabolism; D015398:Signal Transduction
chemical_list: D007473:Ion Channels; D008024:Ligands; D011956:Receptors, Cell Surface; D011950:Receptors, Cholinergic; D011955:Receptors, Drug; D017470:Receptors, Glutamate