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Detection and trapping of intermediate states priming nicotinic receptor channel opening

Author

Listed:
  • Nuriya Mukhtasimova

    (Receptor Biology Laboratory)

  • Won Yong Lee

    (Receptor Biology Laboratory
    Present address: Department of Biology, University of Utah, Salt Lake City, Utah 84112, USA.)

  • Hai-Long Wang

    (Receptor Biology Laboratory)

  • Steven M. Sine

    (Receptor Biology Laboratory
    Mayo Clinic College of Medicine, Rochester, Minnesota 55905, USA)

Abstract

Nicotinic receptor channel opening Acetylcholine receptors are pentameric ligand-gated ion channels that mediate rapid synaptic transmission. Each receptor possesses two agonist-binding sites, whose occupation leads to channel opening, but the precise molecular events that follow agonist binding are unclear. Here, Mukhtasimova et al. covalently lock receptors in conformations equivalent to agonist-bound states, and observe that each binding site initiates the formation of one of two 'primed' states, from which the channels are able to open and close.

Suggested Citation

  • Nuriya Mukhtasimova & Won Yong Lee & Hai-Long Wang & Steven M. Sine, 2009. "Detection and trapping of intermediate states priming nicotinic receptor channel opening," Nature, Nature, vol. 459(7245), pages 451-454, May.
    • Handle: RePEc:nat:nature:v:459:y:2009:i:7245:d:10.1038_nature07923
    DOI: 10.1038/nature07923
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    Cited by:

    1. Christian J. G. Tessier & Johnathon R. Emlaw & Raymond M. Sturgeon & Corrie J. B. daCosta, 2023. "Derepression may masquerade as activation in ligand-gated ion channels," Nature Communications, Nature, vol. 14(1), pages 1-8, December.
    2. Dinesh C Indurthi & Trevor M Lewis & Philip K Ahring & Thomas Balle & Mary Chebib & Nathan L Absalom, 2016. "Ligand Binding at the α4-α4 Agonist-Binding Site of the α4β2 nAChR Triggers Receptor Activation through a Pre-Activated Conformational State," PLOS ONE, Public Library of Science, vol. 11(8), pages 1-20, August.
    3. Chen Fan & John Cowgill & Rebecca J. Howard & Erik Lindahl, 2024. "Divergent mechanisms of steroid inhibition in the human ρ1 GABAA receptor," Nature Communications, Nature, vol. 15(1), pages 1-13, December.

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