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Ligand-gated ion channels (LICs, LGIC), also commonly referred to as ionotropic receptors, are a group of transmembrane ion-channel proteins which open to allow ions such as Na +, K +, Ca 2+, and/or Cl − to pass through the membrane in response to the binding of a chemical messenger (i.e. a ligand), such as a neurotransmitter.
Schematic diagram of an ion channel. 1 - channel domains (typically four per channel), 2 - outer vestibule, 3 - selectivity filter, 4 - diameter of selectivity filter, 5 - phosphorylation site, 6 - cell membrane. Ion channels are pore-forming membrane proteins that allow ions to pass through the channel pore.
Schematic diagram of a GABA A receptor protein ((α1) 2 (β2) 2 (γ2)) which illustrates the five combined subunits that form the protein, the chloride (Cl −) ion channel pore, the two GABA active binding sites at the α1 and β2 interfaces, and the benzodiazepine (BZD) allosteric binding site [20] Side view of the EM structure of the α1β3γ2 GABAA receptor.
Receptor proteins can be classified by their location. Cell surface receptors, also known as transmembrane receptors, include ligand-gated ion channels, G protein-coupled receptors, and enzyme-linked hormone receptors. [1] Intracellular receptors are those found inside the cell, and include cytoplasmic receptors and nuclear receptors. [1]
Schematic diagram of a GABAA receptor protein ((α1)2(β2)2(γ2)) which illustrates the five combined subunits that form the protein, the chloride (Cl-) ion channel pore, the two GABA active binding sites at the α1 and β2 interfaces, and the benzodiazepine (BZD) allosteric binding site at the α1 and γ2 interface.
Diagram of a voltage-sensitive sodium channel α-subunit. G – glycosylation, P – phosphorylation, S – ion selectivity, I – inactivation.Positive (+) charges in S4 are important for transmembrane voltage sensing.
The open conformation of the ion channel allows for the translocation of ions across the cell membrane, while the closed conformation does not. Voltage-gated ion channels are a class of transmembrane proteins that form ion channels that are activated by changes in a cell's electrical membrane potential near the channel. The membrane potential ...
P2X receptor channels transport small monovalent cations, although some also transport Ca 2+. [19] Evidence from early molecular biological and functional studies has strongly indicated that the functional P2X receptor protein is a trimer, with the three peptide subunits arranged around an ion-permeable channel pore. [20]