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Ligand-gated ion channels

Ligand-gated ion channels are a large group of intrinsic transmembrane proteins that allow passage of ions upon activation by a specific ligand.  Most endogenous ligands bind to a site distinct from the ion conduction pore and binding directly causes opening or closing of the channel.  Ligands can bind extracellularly, such as glutamate, ACh and GABA, or intracellularly, such as Ca2+ on Ca2+-activated potassium channels.  Multiple diseases arise from abnormal functioning of ligand-gated ion channels, such as overactivation of NMDA glutamate receptors allows Ca2+ entry, which if uncontrolled leads to activation of the apoptotic pathway and neurotoxicity.

Further reading 

Collingridge et al (2009). A nomenclature for ligand-gated ion channels. Neuropharmacology 56(1) 2 PMID: 18655795

Alexander et al (2011) Guide to Receptors and Channels (GRAC), 5th edition. Br J Pharmacol. 164 Suppl 1 S115 PMID: 22040146

Li et al (2014) Ligand-gated ion channel interacting proteins and their role in neuroprotection. Front. Cell. Neurosci. 8 125 PMID: 24847210

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