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Agonist activation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site

Agonist activation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site

http://www.wikidata.org/entity/Q34804573

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Contrasting properties of α7-selective orthosteric and allosteric agonists examined on native nicotinic acetylcholine receptors Pharmacological Characterisation of Nicotinic Acetylcholine Receptors Expressed in Human iPSC-Derived Neurons Similarities between the Binding Sites of SB-206553 at Serotonin Type 2 and Alpha7 Acetylcholine Nicotinic Receptors: Rationale for Its Polypharmacological Profile Positive modulation of the α9α10 nicotinic cholinergic receptor by ascorbic acid.The Concise Guide to PHARMACOLOGY 2013/14: ligand-gated ion channels.Intrinsically low open probability of α7 nicotinic acetylcholine receptors can be overcome by positive allosteric modulation and serum factors leading to the generation of excitotoxic currents at physiological temperatures ELIC-α7 Nicotinic acetylcholine receptor (α7nAChR) chimeras reveal a prominent role of the extracellular-transmembrane domain interface in allosteric modulation.Changes in temperature have opposing effects on current amplitude in α7 and α4β2 nicotinic acetylcholine receptors.Atomistic insights into human Cys-loop receptors by solution NMR.The Drosophila nicotinic acetylcholine receptor subunits Dα5 and Dα7 form functional homomeric and heteromeric ion channels Nicotinic acetylcholine receptor and the structural basis of neuromuscular transmission: insights from Torpedo postsynaptic membranes Structurally similar allosteric modulators of α7 nicotinic acetylcholine receptors exhibit five distinct pharmacological effects.Subunit interfaces contribute differently to activation and allosteric modulation of neuronal nicotinic acetylcholine receptors.Positive allosteric modulators as an approach to nicotinic acetylcholine receptor-targeted therapeutics: advantages and limitations.An Accessory Agonist Binding Site Promotes Activation of α4β2* Nicotinic Acetylcholine Receptors.Functional Impact of 14 Single Nucleotide Polymorphisms Causing Missense Mutations of Human α7 Nicotinic Receptor.Intramembrane proton binding site linked to activation of bacterial pentameric ion channel.The influence of allosteric modulators and transmembrane mutations on desensitisation and activation of α7 nicotinic acetylcholine receptors A Novel α2/α4 Subtype-selective Positive Allosteric Modulator of Nicotinic Acetylcholine Receptors Acting from the C-tail of an α Subunit Activation of α7 nicotinic receptors by orthosteric and allosteric agonists: influence on single-channel kinetics and conductance Critical Molecular Determinants of α7 Nicotinic Acetylcholine Receptor Allosteric Activation: SEPARATION OF DIRECT ALLOSTERIC ACTIVATION AND POSITIVE ALLOSTERIC MODULATION.A nicotinic acetylcholine receptor transmembrane point mutation (G275E) associated with resistance to spinosad in Frankliniella occidentalis.Emamectin is a non-selective allosteric activator of nicotinic acetylcholine receptors and GABAA/C receptors.Nicotinic acetylcholine receptor antagonists alter the function and expression of serine racemase in PC-12 and 1321N1 cells.Insecticide resistance mediated by an exon skipping event.Microwave-assisted Expeditious and Efficient Synthesis of Cyclopentene Ring-fused Tetrahydroquinoline Derivatives Using Three-component Povarov Reaction.The activity of GAT107, an allosteric activator and positive modulator of α7 nicotinic acetylcholine receptors (nAChR), is regulated by aromatic amino acids that span the subunit interface.Expeditious synthesis, enantiomeric resolution, and enantiomer functional characterization of (4-(4-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide (4BP-TQS): an allosteric agonist-positive allosteric modulator of α7 nicoti NMR structures of the human α7 nAChR transmembrane domain and associated anesthetic binding sites.Targeting neuroinflammation for therapeutic intervention in neurodegenerative pathologies: a role for the peptide analogue of thymulin (PAT).Physical and virtual screening methods for marine toxins and drug discovery targeting nicotinic acetylcholine receptors.Diverse strategies targeting α7 homomeric and α6β2* heteromeric nicotinic acetylcholine receptors for smoking cessation.Targeting brain α7 nicotinic acetylcholine receptors in Alzheimer's disease: rationale and current status.Understanding the Bases of Function and Modulation of α7 Nicotinic Receptors: Implications for Drug Discovery.Competitive binding at a nicotinic receptor transmembrane site of two α7-selective positive allosteric modulators with differing effects on agonist-evoked desensitization.The development of novel polypharmacological agents targeting the multiple binding sites of nicotinic acetylcholine receptors.Orthosteric and allosteric potentiation of heteromeric neuronal nicotinic acetylcholine receptors.Nicotinic acetylcholine receptors at the single-channel level.The desensitization gate of inhibitory Cys-loop receptors.Insights into nicotinic receptor signaling in nicotine addiction: Implications for prevention and treatment.

P2860

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P2860

Agonist activation of alpha7 nicotinic acetylcholine receptors via an allosteric transmembrane site

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2011 nî lūn-bûn

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2011 թուականի Մարտին հրատարակուած գիտական յօդուած

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2011 թվականի մարտին հրատարակված գիտական հոդված

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2011年の論文

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Agonist activation of alpha7 n ...... allosteric transmembrane site

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Agonist activation of alpha7 n ...... allosteric transmembrane site

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Agonist activation of alpha7 n ...... allosteric transmembrane site

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Agonist activation of alpha7 n ...... allosteric transmembrane site

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Agonist activation of alpha7 n ...... allosteric transmembrane site

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PNAS.1017975108

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Proceedings of the National Academy of Sciences of the United States of America

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Agonist activation of alpha7 n ...... allosteric transmembrane site

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P2093

Emanuele Sher

http://www.w3.org/2001/XMLSchema#string

Gareth T Young

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Jaskiran K Gill

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Mari Savolainen

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Neil S Millar

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Ruud Zwart

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P2860

Congenital myasthenic syndrome caused by prolonged acetylcholine receptor channel openings due to a mutation in the M2 domain of the epsilon subunit

Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators

Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors

Crystal structure of the extracellular domain of nAChR alpha1 bound to alpha-bungarotoxin at 1.94 A resolution

ON THE NATURE OF ALLOSTERIC TRANSITIONS: A PLAUSIBLE MODEL

Recent advances in Cys-loop receptor structure and function

Refined structure of the nicotinic acetylcholine receptor at 4A resolution

Allosteric modulation of nicotinic acetylcholine receptors.

Neuronal nicotinic acetylcholine receptors: from the gene to the disease.

Molecular evolution of the nicotinic acetylcholine receptor: an example of multigene family in excitable cells.

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14

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108

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transmembrane protein

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