X-ray structures of general anaesthetics bound to a pentameric ligand-gated ion channel

Hugues Nury, Catherine Van Renterghem, Yun Weng, Alphonso Tran, Marc Baaden, Virginie Dufresne, Jean-Pierre Changeux, James M. Sonner, Marc Delarue () and Pierre-Jean Corringer ()
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Hugues Nury: Institut Pasteur, Groupe Récepteurs-Canaux
Catherine Van Renterghem: Institut Pasteur, Groupe Récepteurs-Canaux
Yun Weng: University of California
Alphonso Tran: University of California
Marc Baaden: Institut de Biologie Physico-Chimique, CNRS UPR 9080
Virginie Dufresne: Institut Pasteur, Groupe Récepteurs-Canaux
Jean-Pierre Changeux: CNRS, URA2182
James M. Sonner: University of California
Marc Delarue: Institut Pasteur, Unité de Dynamique Structurale des Macromolécules
Pierre-Jean Corringer: Institut Pasteur, Groupe Récepteurs-Canaux

Nature, 2011, vol. 469, issue 7330, 428-431

Abstract: Structure of the general anaesthetic site The molecular mechanism of action of general anaesthetics is poorly understood, although there is some evidence that the principal protein targets are pentameric ligand-gated ion channel (pLGICs). The X-ray crystal structures of two common anaesthetics, propofol and desflurane, bound to a bacterial homolog of the pLGIC family have now been determined. The structures reveal that the two anaesthetics bind in the same site — in the upper part of the transmembrane domain of the channel — although desflurane binds deeper inside the ligand-binding cavity. It may be possible to use these structures to design new allosteric modulators that inhibit or potentiate pLGICs at the anaesthetic-binding site.

Date: 2011
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DOI: 10.1038/nature09647

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