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

Author

Listed:
  • Hugues Nury

    (Institut Pasteur, Groupe Récepteurs-Canaux
    CNRS, URA2182
    Institut Pasteur, Unité de Dynamique Structurale des Macromolécules
    CNRS, URA2185)

  • Catherine Van Renterghem

    (Institut Pasteur, Groupe Récepteurs-Canaux
    CNRS, URA2182)

  • 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
    CNRS, URA2182)

  • Jean-Pierre Changeux

    (CNRS, URA2182
    Collège de France)

  • James M. Sonner

    (University of California)

  • Marc Delarue

    (Institut Pasteur, Unité de Dynamique Structurale des Macromolécules
    CNRS, URA2185)

  • Pierre-Jean Corringer

    (Institut Pasteur, Groupe Récepteurs-Canaux
    CNRS, URA2182)

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.

Suggested Citation

  • Hugues Nury & Catherine Van Renterghem & Yun Weng & Alphonso Tran & Marc Baaden & Virginie Dufresne & Jean-Pierre Changeux & James M. Sonner & Marc Delarue & Pierre-Jean Corringer, 2011. "X-ray structures of general anaesthetics bound to a pentameric ligand-gated ion channel," Nature, Nature, vol. 469(7330), pages 428-431, January.
    • Handle: RePEc:nat:nature:v:469:y:2011:i:7330:d:10.1038_nature09647
    DOI: 10.1038/nature09647
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    Cited by:

    1. Letícia Stock & Juliana Hosoume & Leonardo Cirqueira & Werner Treptow, 2018. "Binding of the general anesthetic sevoflurane to ion channels," PLOS Computational Biology, Public Library of Science, vol. 14(11), pages 1-23, November.
    2. Nikhil Bharambe & Zhuowen Li & David Seiferth & Asha Manikkoth Balakrishna & Philip C. Biggin & Sandip Basak, 2024. "Cryo-EM structures of prokaryotic ligand-gated ion channel GLIC provide insights into gating in a lipid environment," Nature Communications, Nature, vol. 15(1), pages 1-16, December.
    3. John T. Petroff & Noah M. Dietzen & Ezry Santiago-McRae & Brett Deng & Maya S. Washington & Lawrence J. Chen & K. Trent Moreland & Zengqin Deng & Michael Rau & James A. J. Fitzpatrick & Peng Yuan & Th, 2022. "Open-channel structure of a pentameric ligand-gated ion channel reveals a mechanism of leaflet-specific phospholipid modulation," Nature Communications, Nature, vol. 13(1), pages 1-16, December.

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