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Curr Opin Physiol. 2019 Jun 12;2:19-26. doi: 10.1016/j.cophys.2017.12.012.

A tale of ligands big and small: an update on how pentameric ligand-gated ion channels interact with agonists and proteins.

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Center for Biopharmaceuticals, Department of Drug Design and Pharmacology, University of Copenhagen, 2100 Copenhagen, Denmark.
Department of Neuroscience, Physiology and Pharmacology, Division of Biosciences, University College London, Gower St, London WC1E 6BT, United Kingdom.


Pentameric ligand-gated ion channels (pLGICs, also known as Cys-loop receptors) are a large family of ion channels expressed in all Bilateria and in several groups of bacteria and archaea. They are activated by small-molecule neurotransmitters to mediate fast transmission at many central and peripheral nervous system synapses and are the target of several drugs and insecticides. Here we review recent advances in the field, focussing on new insights on the structure of the agonist-binding site and on newly discovered protein-protein interactions involving pLGICs.


Ion channel; auxiliary subunit; chaperone; ligand binding; membrane protein function; toxin

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