Ligand-gated ion channels function as rapid signal transducers, converting chemical signals (in the form of neurotransmitters) into electrical signals in the postsynaptic neuron. This is achieved by the recognition of neurotransmitter at its specific-binding sites, which then triggers the opening of an ion channel (‘gating’). For this to occur rapidly (<1 ms), there must be an efficient coupling between the agonist-binding site and the gate, located more than 30 Å (1 Å=0.1 nm) away. Whereas a great deal of progress has been made in elucidating the structure and function of both the agonist-binding site and the ion permeation pathway in ligand-gated ion channels, our knowledge of the coupling mechanism between these domains has been limited. In this review, we summarize recent studies of the agonist-binding site and the ion channel in the γ-aminobutyric acid type A receptor, and discuss those structural elements that may mediate coupling between them. We will also consider some possible molecular mechanisms of receptor activation.
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June 01 2004
Structural elements involved in activation of the γ-aminobutyric acid type A (GABAA) receptor
T.L. Kash;
T.L. Kash
*Graduate Program in Neuroscience, Weill Graduate School of Biomedical Sciences, Cornell University, New York, NY 10021, U.S.A.
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J.R. Trudell;
J.R. Trudell
†Department of Anesthesia and Beckman Program for Molecular and Genetic Medicine, Stanford University, Stanford, CA 94305-5117, U.S.A.
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N.L. Harrison
N.L. Harrison
1
‡Departments of Anesthesiology and Pharmacology, Weill Medical College, Cornell University, New York, NY 10021, U.S.A.
1To whom correspondence should be addressed (email [email protected]).
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Publisher: Portland Press Ltd
Online ISSN: 1470-8752
Print ISSN: 0300-5127
© 2004 Biochemical Society
2004
Biochem Soc Trans (2004) 32 (3): 540–546.
Citation
T.L. Kash, J.R. Trudell, N.L. Harrison; Structural elements involved in activation of the γ-aminobutyric acid type A (GABAA) receptor. Biochem Soc Trans 1 June 2004; 32 (3): 540–546. doi: https://doi.org/10.1042/bst0320540
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