Structure and Function of Ligand-Gated Channels
The ligand-gated ion channel family is responsible for fast excitatory and inhibitory synaptic transmission throughout the brain. Inhibition is mediated by GABAA and glycine receptors, whereas excitation is mediated by nicotinic acetylcholine, serotonin, and glutamate receptors. The ligand-gated ion channel receptors possess multiple ligand-binding sites and consist of multiple subunits that are assembled in various combinations to impart different pharmacological and kinetic properties to the channel. These subunits share approximately 50% to 70% sequence homology within their individual receptor class and share approximately 15% to 40% homology across classes. Each subunit contains four distinct hydrophobic regions that may constitute transmembrane domains of these receptor subunits. This chapter discusses transmembrane structure, glutamate receptor families, structural determinants of permeation and channel block, structural determinants of modulation, and functional significance of molecular diversity in glutamate receptors.
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