ArticleBiochemistry2010
Conformational changes in the nicotinic acetylcholine receptor during gating and desensitization.
Article in Biochemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 36 citations in OpenAlex.
- Protein Painting Mass Spectrometry in the Discovery of Interaction Sites within the Acetylcholine Binding Protein.ACS chemical neuroscience · 2024Article
- Nicotinic receptor pharmacology in silico: Insights and challenges.Neuropharmacology · 2020Review
- The dual-gate model for pentameric ligand-gated ion channels activation and desensitization.The Journal of physiology · 2018Review
- Enantiomeric barbiturates bind distinct inter- and intrasubunit binding sites in a nicotinic acetylcholine receptor (nAChR).The Journal of biological chemistry · 2017Article
- Trapping of ivermectin by a pentameric ligand-gated ion channel upon open-to-closed isomerization.Scientific reports · 2017Article
- Mutational Analysis at Intersubunit Interfaces of an Anionic Glutamate Receptor Reveals a Key Interaction Important for Channel Gating by Ivermectin.Frontiers in molecular neuroscience · 2017Article
- Desformylflustrabromine (dFBr) and [3H]dFBr-Labeled Binding Sites in a Nicotinic Acetylcholine Receptor.Molecular pharmacology · 2015Article
- The effect of BLA GABA(A) receptors in anxiolytic-like effect and aversive memory deficit induced by ACPA.EXCLI journal · 2015Article
- Photoaffinity labeling of nicotinic receptors: diversity of drug binding sites!Journal of molecular neuroscience : MN · 2014Review
- Photoaffinity labeling the propofol binding site in GLIC.Biochemistry · 2014Article
- Crosslinking constraints and computational models as complementary tools in modeling the extracellular domain of the glycine receptor.PloS one · 2014Article
- Insights into distinct modulation of α7 and α7β2 nicotinic acetylcholine receptors by the volatile anesthetic isoflurane.The Journal of biological chemistry · 2013Article
- Site-directed spin labeling reveals pentameric ligand-gated ion channel gating motions.PLoS biology · 2013Article
- Intermediate closed state for glycine receptor function revealed by cysteine cross-linking.Proceedings of the National Academy of Sciences of the United States of America · 2013Article
- Inhibition versus potentiation of ligand-gated ion channels can be altered by a single mutation that moves ligands between intra- and intersubunit sites.Structure (London, England : 1993) · 2013Article
- Identification of propofol binding sites in a nicotinic acetylcholine receptor with a photoreactive propofol analog.The Journal of biological chemistry · 2013Article
- A locally closed conformation of a bacterial pentameric proton-gated ion channel.Nature structural & molecular biology · 2012Article
- Article
- Mapping general anesthetic binding site(s) in human α1β3 γ-aminobutyric acid type A receptors with [³H]TDBzl-etomidate, a photoreactive etomidate analogue.Biochemistry · 2012Article
- Activation and desensitization induce distinct conformational changes at the extracellular-transmembrane domain interface of the glycine receptor.The Journal of biological chemistry · 2011Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
The nicotinic acetylcholine receptor (nAChR) is a member of the important Cys loop ligand-gated ion channel superfamily that modulates neuronal excitability. After they respond to their agonists, their actions are terminated either by removal of ligand or by fast and slow desensitization, processes that play an important role in modulating the duration of conducting states and hence of integrated neuronal behavior. We monitored structural changes occurring during fast and slow desensitization in the transmembrane domain of the Torpedo nAChR using time-resolved photolabeling with the hydrophobic probe 3-(trifluoromethyl)-3-(m-iodophenyl)diazirine (TID). After channel opening, TID photolabels a residue on the delta-subunit's M2-M3 loop and a cluster of four residues on deltaM1 and deltaM2, defining an open state pocket [Arevalo, E., et al. (2005) J. Biol. Chem. 280, 13631-13640]. We now find that photolabeling of this pocket persists during the transition to the fast desensitized state, the extent of photoincorporation decreasing only with the transition to the slow desensitized state. In contrast, the extent of photoincorporation in the channel lumen at the conserved 9'-leucines on the second transmembrane helix (M2-9') decreased successively during the resting to open and open to fast desensitized state transitions, implying that the local conformation is different in each state, a conclusion consistent with the hypothesis that there are separate gates for channel opening and desensitization. Thus, although during fast desensitization there is a conformation change in the channel lumen at the level of M2-9', there is none in the regions of the delta-subunit's M2-M3 loop and the interior of its M1-M4 helix bundle until slow desensitization occurs.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.