ArticleBritish journal of pharmacology2005
Key roles of hydrophobic rings of TM2 in gating of the alpha9alpha10 nicotinic cholinergic receptor.
Article in British journal of pharmacology, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 29 citations in OpenAlex.
- Challenges and lessons learned in attempts to develop in vitro models for ultrasound neuromodulation using local field potential measurements in hippocampal tissue.Biophysical journal · 2025Article
- Virally mediated enhancement of efferent inhibition reduces acoustic trauma in wild-type murine cochleas.Molecular therapy. Methods & clinical development · 2025Article
- Human α10 nicotinic acetylcholine receptor subunits assemble to form functional receptors.The Journal of biological chemistry · 2025Article
- Key role of the TM2-TM3 loop in calcium potentiation of the α9α10 nicotinic acetylcholine receptor.Cellular and molecular life sciences : CMLS · 2024Article
- When is a hydrophobic gate not a hydrophobic gate?The Journal of general physiology · 2022Article
- The α9α10 nicotinic acetylcholine receptor: a compelling drug target for hearing loss?Expert opinion on therapeutic targets · 2022Review
- Water in Nanopores and Biological Channels: A Molecular Simulation Perspective.Chemical reviews · 2020Review
- Attenuation in Nicotinic Acetylcholine Receptor α9 and α10 Subunit Double Knock-Out Mice of Experimental Autoimmune Encephalomyelitis.Biomolecules · 2019Article
- A Gain-of-Function Mutation in the α9 Nicotinic Acetylcholine Receptor Alters Medial Olivocochlear Efferent Short-Term Synaptic Plasticity.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2018Article
- Commentary: Nicotinic Acetylcholine Receptor α9 and α10 Subunits Are Expressed in the Brain of Mice.Frontiers in cellular neuroscience · 2018Article
- α2* Nicotinic acetylcholine receptors influence hippocampus-dependent learning and memory in adolescent mice.Learning & memory (Cold Spring Harbor, N.Y.) · 2017Article
- Tracking the molecular evolution of calcium permeability in a nicotinic acetylcholine receptor.Molecular biology and evolution · 2014Article
- Ultrastructure of cisternal synapses on outer hair cells of the mouse cochlea.The Journal of comparative neurology · 2014Article
- Positive modulation of the α9α10 nicotinic cholinergic receptor by ascorbic acid.British journal of pharmacology · 2013Article
- Mutations that stabilize the open state of the Erwinia chrisanthemi ligand-gated ion channel fail to change the conformation of the pore domain in crystals.Proceedings of the National Academy of Sciences of the United States of America · 2012Article
- Structural basis of activation of cys-loop receptors: the extracellular-transmembrane interface as a coupling region.Molecular neurobiology · 2009Review
- A point mutation in the hair cell nicotinic cholinergic receptor prolongs cochlear inhibition and enhances noise protection.PLoS biology · 2009Article
- Stoichiometry of the alpha9alpha10 nicotinic cholinergic receptor.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2005Article
- Modeling interactions between voltage-gated Ca (2+) channels and KCa1.1 channels.Channels (Austin, Tex.)Article
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Authors and funding
8 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We have performed a systematic mutagenesis of three hydrophobic rings (17', 13' and 9') within transmembrane region (TM) 2 of the alpha9alpha10 nicotinic cholinergic receptor (nAChR) to a hydrophilic (threonine) residue and compared the properties of mutant receptors reconstituted in Xenopus laevis oocytes. Phenotypic changes in alpha9alpha10 mutant receptors were evidenced by a decrease in the desensitization rate, an increase in both the EC(50) for ACh as well as the efficacy of partial agonists and the reduction of the allosteric modulation by extracellular Ca(2+). Mutated receptors exhibited spontaneous openings and, at the single-channel level, an increased apparent mean open time with no major changes in channel conductance, thus suggesting an increase in gating of the channel as the underlying mechanism. Overall, the degrees of the phenotypes of mutant receptors were more overt in the case of the centrally located V13'T mutant. Based on the atomic model of the pore of the electric organ of the Torpedo ray, we can propose that the interactions of side chains at positions 13' and 9' are key ones in creating an energetic barrier to ion permeation. In spite of the fact that the roles of the TM2 residues are mostly conserved in the distant alpha9alpha10 member of the nAChR family, their mechanistic contributions to channel gating show significant differences when compared to other nAChRs. These differences might be originated from slight differential intramolecular rearrangements during gating for the different receptors and might lead each nAChR to be in tune with their physiological roles.
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