Crystal structures of a pentameric ligand-gated ion channel provide a mechanism for activation.

PubWeight™: 1.32‹?› | Rank: Top 10%

🔗 View Article (PMC 3903189)

Published in Proc Natl Acad Sci U S A on December 23, 2013

Authors

Ludovic Sauguet1, Azadeh Shahsavar, Frédéric Poitevin, Christèle Huon, Anaïs Menny, Àkos Nemecz, Ahmed Haouz, Jean-Pierre Changeux, Pierre-Jean Corringer, Marc Delarue

Author Affiliations

1: Unité de Dynamique Structurale des Macromolécules, Unité Mixte de Recherche (UMR) 3528 du Centre National de la Recherche Scientifique (CNRS), Institut Pasteur, 75015 Paris, France.

Articles citing this

X-ray structure of the mouse serotonin 5-HT3 receptor. Nature (2014) 1.67

X-ray structures of GluCl in apo states reveal a gating mechanism of Cys-loop receptors. Nature (2014) 1.46

Signal Transduction at the Domain Interface of Prokaryotic Pentameric Ligand-Gated Ion Channels. PLoS Biol (2016) 1.42

Glycine receptor mechanism elucidated by electron cryo-microscopy. Nature (2015) 1.41

Mechanism of activation of the prokaryotic channel ELIC by propylamine: a single-channel study. J Gen Physiol (2015) 1.08

Hydrophobic gating in ion channels. J Mol Biol (2014) 1.00

Catch-and-hold activation of muscle acetylcholine receptors having transmitter binding site mutations. Biophys J (2014) 0.95

Allosteric and hyperekplexic mutant phenotypes investigated on an α1 glycine receptor transmembrane structure. Proc Natl Acad Sci U S A (2015) 0.94

Conformational Changes Underlying Desensitization of the Pentameric Ligand-Gated Ion Channel ELIC. Structure (2015) 0.88

Iterative phasing for fluctuation X-ray scattering. Proc Natl Acad Sci U S A (2015) 0.88

ELIC-α7 Nicotinic acetylcholine receptor (α7nAChR) chimeras reveal a prominent role of the extracellular-transmembrane domain interface in allosteric modulation. J Biol Chem (2014) 0.86

Structural requirements in the transmembrane domain of GLIC revealed by incorporation of noncanonical histidine analogs. Chem Biol (2014) 0.84

Structural Basis for Xenon Inhibition in a Cationic Pentameric Ligand-Gated Ion Channel. PLoS One (2016) 0.83

Role of the Fourth Transmembrane α Helix in the Allosteric Modulation of Pentameric Ligand-Gated Ion Channels. Structure (2015) 0.82

Principles of agonist recognition in Cys-loop receptors. Front Physiol (2014) 0.82

Correlating structural and energetic changes in glycine receptor activation. J Biol Chem (2015) 0.81

Function of the M1 π-helix in endplate receptor activation and desensitization. J Physiol (2015) 0.81

Structural mechanisms of activation and desensitization in neurotransmitter-gated ion channels. Nat Struct Mol Biol (2016) 0.81

Atomistic insights into human Cys-loop receptors by solution NMR. Biochim Biophys Acta (2014) 0.80

Allosteric regulation of pentameric ligand-gated ion channels: an emerging mechanistic perspective. Channels (Austin) (2014) 0.80

Protein dynamics and the allosteric transitions of pentameric receptor channels. Biophys Rev (2014) 0.79

A combined coarse-grained and all-atom simulation of TRPV1 channel gating and heat activation. J Gen Physiol (2015) 0.79

The M4 Transmembrane α-Helix Contributes Differently to Both the Maturation and Function of Two Prokaryotic Pentameric Ligand-gated Ion Channels. J Biol Chem (2015) 0.78

Intramembrane aromatic interactions influence the lipid sensitivities of pentameric ligand-gated ion channels. J Biol Chem (2014) 0.78

Ethanol Modulation is Quantitatively Determined by the Transmembrane Domain of Human α1 Glycine Receptors. Alcohol Clin Exp Res (2015) 0.77

Structural Studies of GABAA Receptor Binding Sites: Which Experimental Structure Tells us What? Front Mol Neurosci (2016) 0.77

Potentiation of Gamma Aminobutyric Acid Receptors (GABAAR) by Ethanol: How Are Inhibitory Receptors Affected? Front Cell Neurosci (2016) 0.77

Inter-subunit disulfide locking of the human P2X3 receptor elucidates ectodomain movements associated with channel gating. Purinergic Signal (2016) 0.77

A chimeric prokaryotic pentameric ligand-gated channel reveals distinct pathways of activation. J Gen Physiol (2015) 0.76

Prediction and validation of protein intermediate states from structurally rich ensembles and coarse-grained simulations. Nat Commun (2016) 0.76

EPR Studies of Gating Mechanisms in Ion Channels. Methods Enzymol (2015) 0.76

Structure and Pharmacologic Modulation of Inhibitory Glycine Receptors. Mol Pharmacol (2016) 0.76

A Structural Model of the Human α7 Nicotinic Receptor in an Open Conformation. PLoS One (2015) 0.76

Structural basis for cooperative interactions of substituted 2-aminopyrimidines with the acetylcholine binding protein. Proc Natl Acad Sci U S A (2014) 0.76

Long distance effect on ligand-gated ion channels extracellular domain may affect interactions with the intracellular machinery. Commun Integr Biol (2014) 0.76

Functional characterization of neurotransmitter activation and modulation in a nematode model ligand-gated ion channel. J Neurochem (2016) 0.75

Discovery, synthesis, biological evaluation and structure-based optimization of novel piperidine derivatives as acetylcholine-binding protein ligands. Acta Pharmacol Sin (2016) 0.75

Functional and Biochemical Characterization of Alvinella pompejana Cys-Loop Receptor Homologues. PLoS One (2016) 0.75

Crystal structure and dynamics of a lipid-induced potential desensitized-state of a pentameric ligand-gated channel. Elife (2017) 0.75

Identification of a pre-active conformation of a pentameric channel receptor. Elife (2017) 0.75

Allosteric binding site in a Cys-loop receptor ligand-binding domain unveiled in the crystal structure of ELIC in complex with chlorpromazine. Proc Natl Acad Sci U S A (2016) 0.75

A mechanism for acetylcholine receptor gating based on structure, coupling, phi, and flip. J Gen Physiol (2016) 0.75

Perturbation of Critical Prolines in Gloeobacter violaceus Ligand-gated Ion Channel (GLIC) Supports Conserved Gating Motions among Cys-loop Receptors. J Biol Chem (2015) 0.75

A chimeric prokaryotic-eukaryotic pentameric ligand gated ion channel reveals interactions between the extracellular and transmembrane domains shape neurosteroid modulation. Neuropharmacology (2017) 0.75

Ketamine Inhibition of the Pentameric Ligand-Gated Ion Channel GLIC. Biophys J (2017) 0.75

A cost-effective protocol for the over-expression and purification of fully-functional and more stable Erwinia chrysanthemi ligand-gated ion channel. Protein Expr Purif (2017) 0.75

Articles cited by this

Refined structure of the nicotinic acetylcholine receptor at 4A resolution. J Mol Biol (2005) 12.16

Nicotine and carbamylcholine binding to nicotinic acetylcholine receptors as studied in AChBP crystal structures. Neuron (2004) 7.48

X-ray structure of a prokaryotic pentameric ligand-gated ion channel. Nature (2008) 6.02

Principles of activation and permeation in an anion-selective Cys-loop receptor. Nature (2011) 5.93

X-ray structure of a pentameric ligand-gated ion channel in an apparently open conformation. Nature (2008) 5.77

Structures of Aplysia AChBP complexes with nicotinic agonists and antagonists reveal distinctive binding interfaces and conformations. EMBO J (2005) 5.55

Structure of a potentially open state of a proton-activated pentameric ligand-gated ion channel. Nature (2008) 5.09

Principal pathway coupling agonist binding to channel gating in nicotinic receptors. Nature (2005) 3.47

A prokaryotic proton-gated ion channel from the nicotinic acetylcholine receptor family. Nature (2006) 3.04

X-ray structures of general anaesthetics bound to a pentameric ligand-gated ion channel. Nature (2011) 3.00

Normal mode analysis suggests a quaternary twist model for the nicotinic receptor gating mechanism. Biophys J (2005) 2.33

Low-resolution refinement tools in REFMAC5. Acta Crystallogr D Biol Crystallogr (2012) 2.11

One-microsecond molecular dynamics simulation of channel gating in a nicotinic receptor homologue. Proc Natl Acad Sci U S A (2010) 1.81

Pore opening and closing of a pentameric ligand-gated ion channel. Proc Natl Acad Sci U S A (2010) 1.71

Structure and pharmacology of pentameric receptor channels: from bacteria to brain. Structure (2012) 1.69

A locally closed conformation of a bacterial pentameric proton-gated ion channel. Nat Struct Mol Biol (2012) 1.56

Protein structural change upon ligand binding: linear response theory. Phys Rev Lett (2005) 1.53

Structural determinants in phycotoxins and AChBP conferring high affinity binding and nicotinic AChR antagonism. Proc Natl Acad Sci U S A (2010) 1.48

A solution NMR study showing that active site ligands and nucleotides directly perturb the allosteric equilibrium in aspartate transcarbamoylase. Proc Natl Acad Sci U S A (2007) 1.46

A new era of GPCR structural and chemical biology. Nat Chem Biol (2012) 1.41

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. Proc Natl Acad Sci U S A (2012) 1.38

Backbone mutations in transmembrane domains of a ligand-gated ion channel: implications for the mechanism of gating. Cell (1999) 1.37

Structural basis for ion permeation mechanism in pentameric ligand-gated ion channels. EMBO J (2013) 1.37

Structural basis for potentiation by alcohols and anaesthetics in a ligand-gated ion channel. Nat Commun (2013) 1.35

Acetylcholine receptor gating at extracellular transmembrane domain interface: the "pre-M1" linker. J Gen Physiol (2007) 1.33

Structure of the M2 transmembrane segment of GLIC, a prokaryotic Cys loop receptor homologue from Gloeobacter violaceus, probed by substituted cysteine accessibility. J Biol Chem (2011) 1.33

Identification of calcium binding sites that regulate potentiation of a neuronal nicotinic acetylcholine receptor. EMBO J (1996) 1.25

Multisite binding of a general anesthetic to the prokaryotic pentameric Erwinia chrysanthemi ligand-gated ion channel (ELIC). J Biol Chem (2013) 1.22

Pentameric ligand-gated ion channel ELIC is activated by GABA and modulated by benzodiazepines. Proc Natl Acad Sci U S A (2012) 1.22

Ion channel gating: a first-passage time analysis of the Kramers type. Proc Natl Acad Sci U S A (2002) 1.21

50 years of allosteric interactions: the twists and turns of the models. Nat Rev Mol Cell Biol (2013) 1.17

A gating mechanism of pentameric ligand-gated ion channels. Proc Natl Acad Sci U S A (2013) 1.15

The α1K276E startle disease mutation reveals multiple intermediate states in the gating of glycine receptors. J Neurosci (2012) 1.13

Thinking in cycles: MWC is a good model for acetylcholine receptor-channels. J Physiol (2011) 1.13

Desensitization mechanism in prokaryotic ligand-gated ion channel. J Biol Chem (2012) 1.07

Crystal structure of the extracellular domain of a bacterial ligand-gated ion channel. J Mol Biol (2009) 1.07

Conformational transitions underlying pore opening and desensitization in membrane-embedded Gloeobacter violaceus ligand-gated ion channel (GLIC). J Biol Chem (2012) 1.04

Predicting order of conformational changes during protein conformational transitions using an interpolated elastic network model. Proteins (2010) 1.02

Entropic mechanism of large fluctuation in allosteric transition. Proc Natl Acad Sci U S A (2010) 0.98

Inhibition of the prokaryotic pentameric ligand-gated ion channel ELIC by divalent cations. PLoS Biol (2012) 0.96

Decrypting the sequence of structural events during the gating transition of pentameric ligand-gated ion channels based on an interpolated elastic network model. PLoS Comput Biol (2011) 0.94

Packing of the extracellular domain hydrophobic core has evolved to facilitate pentameric ligand-gated ion channel function. J Biol Chem (2010) 0.88

Effect of cobratoxin binding on the normal mode vibration within acetylcholine binding protein. J Chem Inf Model (2008) 0.86

Coarse-grained and all-atom modeling of structural states and transitions in hemoglobin. Proteins (2012) 0.86

Computing free energy of a large-scale allosteric transition in adenylate kinase using all atom explicit solvent simulations. J Phys Chem B (2012) 0.83

Articles by these authors

X-ray structure of a pentameric ligand-gated ion channel in an apparently open conformation. Nature (2008) 5.77

Conscious, preconscious, and subliminal processing: a testable taxonomy. Trends Cogn Sci (2006) 4.66

Experimental and theoretical approaches to conscious processing. Neuron (2011) 4.28

Nicotinic receptors: allosteric transitions and therapeutic targets in the nervous system. Nat Rev Drug Discov (2009) 3.26

A prokaryotic proton-gated ion channel from the nicotinic acetylcholine receptor family. Nature (2006) 3.04

X-ray structures of general anaesthetics bound to a pentameric ligand-gated ion channel. Nature (2011) 3.00

Subunit composition of functional nicotinic receptors in dopaminergic neurons investigated with knock-out mice. J Neurosci (2003) 2.85

A neuronal network model linking subjective reports and objective physiological data during conscious perception. Proc Natl Acad Sci U S A (2003) 2.79

Hierarchical control of dopamine neuron-firing patterns by nicotinic receptors. Neuron (2006) 2.69

Normal mode analysis suggests a quaternary twist model for the nicotinic receptor gating mechanism. Biophys J (2005) 2.33

NOMAD-Ref: visualization, deformation and refinement of macromolecular structures based on all-atom normal mode analysis. Nucleic Acids Res (2006) 2.21

The diversity of subunit composition in nAChRs: evolutionary origins, physiologic and pharmacologic consequences. J Neurobiol (2002) 2.20

Anesthetic sensitivity of the Gloeobacter violaceus proton-gated ion channel. Anesth Analg (2009) 2.15

Distribution and pharmacology of alpha 6-containing nicotinic acetylcholine receptors analyzed with mutant mice. J Neurosci (2002) 2.05

Nicotine upregulates its own receptors through enhanced intracellular maturation. Neuron (2005) 1.89

One-microsecond molecular dynamics simulation of channel gating in a nicotinic receptor homologue. Proc Natl Acad Sci U S A (2010) 1.81

Models of the extracellular domain of the nicotinic receptors and of agonist- and Ca2+-binding sites. Proc Natl Acad Sci U S A (2002) 1.78

The beta2 but not alpha7 subunit of the nicotinic acetylcholine receptor is required for nicotine-conditioned place preference in mice. Psychopharmacology (Berl) (2006) 1.76

Structure and pharmacology of pentameric receptor channels: from bacteria to brain. Structure (2012) 1.69

Molecular tuning of fast gating in pentameric ligand-gated ion channels. Proc Natl Acad Sci U S A (2005) 1.58

A locally closed conformation of a bacterial pentameric proton-gated ion channel. Nat Struct Mol Biol (2012) 1.56

Structural basis of potent Zika-dengue virus antibody cross-neutralization. Nature (2016) 1.52

Structural basis for alcohol modulation of a pentameric ligand-gated ion channel. Proc Natl Acad Sci U S A (2011) 1.52

A neuronal model of predictive coding accounting for the mismatch negativity. J Neurosci (2012) 1.48

Ongoing spontaneous activity controls access to consciousness: a neuronal model for inattentional blindness. PLoS Biol (2005) 1.47

Peptides targeting the PDZ domain of PTPN4 are efficient inducers of glioblastoma cell death. Structure (2011) 1.46

PDB_Hydro: incorporating dipolar solvents with variable density in the Poisson-Boltzmann treatment of macromolecule electrostatics. Nucleic Acids Res (2006) 1.45

Structural plasticity and catalysis regulation of a thermosensor histidine kinase. Proc Natl Acad Sci U S A (2009) 1.45

Distinct contributions of nicotinic acetylcholine receptor subunit alpha4 and subunit alpha6 to the reinforcing effects of nicotine. Proc Natl Acad Sci U S A (2011) 1.44

Executive and social behaviors under nicotinic receptor regulation. Proc Natl Acad Sci U S A (2003) 1.44

Altered map of visual space in the superior colliculus of mice lacking early retinal waves. J Neurosci (2005) 1.38

Atomic structure and dynamics of pentameric ligand-gated ion channels: new insight from bacterial homologues. J Physiol (2009) 1.38

Structural basis for ion permeation mechanism in pentameric ligand-gated ion channels. EMBO J (2013) 1.37

The crystal structure of the mouse apoptosis-inducing factor AIF. Nat Struct Biol (2002) 1.36

Incorporating dipolar solvents with variable density in Poisson-Boltzmann electrostatics. Biophys J (2008) 1.36

Structural basis for potentiation by alcohols and anaesthetics in a ligand-gated ion channel. Nat Commun (2013) 1.35

Structural insights into the quinolone resistance mechanism of Mycobacterium tuberculosis DNA gyrase. PLoS One (2010) 1.35

Functional prokaryotic-eukaryotic chimera from the pentameric ligand-gated ion channel family. Proc Natl Acad Sci U S A (2011) 1.34

Implications of the quaternary twist allosteric model for the physiology and pathology of nicotinic acetylcholine receptors. Proc Natl Acad Sci U S A (2006) 1.32

Experimentally based model of a complex between a snake toxin and the alpha 7 nicotinic receptor. Proc Natl Acad Sci U S A (2002) 1.32

MinActionPath: maximum likelihood trajectory for large-scale structural transitions in a coarse-grained locally harmonic energy landscape. Nucleic Acids Res (2007) 1.32

Conformational selection or induced fit? 50 years of debate resolved. F1000 Biol Rep (2011) 1.31

Pore conformations and gating mechanism of a Cys-loop receptor. Proc Natl Acad Sci U S A (2005) 1.31

Nicotine and serotonin in immune regulation and inflammatory processes: a perspective. J Leukoc Biol (2006) 1.22

Pentameric ligand-gated ion channel ELIC is activated by GABA and modulated by benzodiazepines. Proc Natl Acad Sci U S A (2012) 1.22

AquaSAXS: a web server for computation and fitting of SAXS profiles with non-uniformally hydrated atomic models. Nucleic Acids Res (2011) 1.20

An H-bond between two residues from different loops of the acetylcholine binding site contributes to the activation mechanism of nicotinic receptors. EMBO J (2003) 1.19

Localization of [3H]nicotine, [3H]cytisine, [3H]epibatidine, and [125I]alpha-bungarotoxin binding sites in the brain of Macaca mulatta. J Comp Neurol (2003) 1.18

Monitoring protein interactions in the living cell through the fluorescence decays of the cyan fluorescent protein. Chemphyschem (2006) 1.18

Rapsyn escorts the nicotinic acetylcholine receptor along the exocytic pathway via association with lipid rafts. J Neurosci (2002) 1.17

Nicotine activates immature "silent" connections in the developing hippocampus. Proc Natl Acad Sci U S A (2003) 1.17

3D structure and allosteric modulation of the transmembrane domain of pentameric ligand-gated ion channels. Neuropharmacology (2010) 1.16

A gating mechanism of pentameric ligand-gated ion channels. Proc Natl Acad Sci U S A (2013) 1.15

Intracellular complexes of the beta2 subunit of the nicotinic acetylcholine receptor in brain identified by proteomics. Proc Natl Acad Sci U S A (2007) 1.15

An extracellular protein microdomain controls up-regulation of neuronal nicotinic acetylcholine receptors by nicotine. J Biol Chem (2004) 1.15

α-Conotoxin BuIA[T5A;P6O]: a novel ligand that discriminates between α6ß4 and α6ß2 nicotinic acetylcholine receptors and blocks nicotine-stimulated norepinephrine release. FASEB J (2010) 1.12

Nicotinic modulation of network and synaptic transmission in the immature hippocampus investigated with genetically modified mice. J Physiol (2006) 1.12

Biological and structural characterization of the Mycobacterium smegmatis nitroreductase NfnB, and its role in benzothiazinone resistance. Mol Microbiol (2010) 1.12

Refinement of docked protein-ligand and protein-DNA structures using low frequency normal mode amplitude optimization. Nucleic Acids Res (2005) 1.11

Prefrontal nicotinic receptors control novel social interaction between mice. FASEB J (2011) 1.11

Alterations of cortical pyramidal neurons in mice lacking high-affinity nicotinic receptors. Proc Natl Acad Sci U S A (2010) 1.10

Interplay of beta2* nicotinic receptors and dopamine pathways in the control of spontaneous locomotion. Proc Natl Acad Sci U S A (2008) 1.08

Reinforcing effects of nicotine microinjections into the ventral tegmental area of mice: dependence on cholinergic nicotinic and dopaminergic D1 receptors. Neuropharmacology (2006) 1.08

Long-term effects of chronic nicotine exposure on brain nicotinic receptors. Proc Natl Acad Sci U S A (2007) 1.08

Perinatal exposure to nicotine causes deficits associated with a loss of nicotinic receptor function. Proc Natl Acad Sci U S A (2005) 1.08

Crystal structure of the extracellular domain of a bacterial ligand-gated ion channel. J Mol Biol (2009) 1.07

Knockout and knockin mice to investigate the role of nicotinic receptors in the central nervous system. Prog Brain Res (2004) 1.05

Heterogeneity and selective targeting of neuronal nicotinic acetylcholine receptor (nAChR) subtypes expressed on retinal afferents of the superior colliculus and lateral geniculate nucleus: identification of a new native nAChR subtype alpha3beta2(alpha5 or beta3) enriched in retinocollicular afferents. Mol Pharmacol (2005) 1.05

The emergence of human consciousness: from fetal to neonatal life. Pediatr Res (2009) 1.04

Electron microscopic evidence for nucleation and growth of 3D acetylcholine receptor microcrystals in structured lipid-detergent matrices. Proc Natl Acad Sci U S A (2003) 1.03

AQUASOL: An efficient solver for the dipolar Poisson-Boltzmann-Langevin equation. J Chem Phys (2010) 1.03

Genome-wide regulon and crystal structure of BlaI (Rv1846c) from Mycobacterium tuberculosis. Mol Microbiol (2009) 1.03

Beta2-containing nicotinic receptors contribute to the organization of sleep and regulate putative micro-arousals in mice. J Neurosci (2004) 1.02

DARPin-assisted crystallography of the CC2-LZ domain of NEMO reveals a coupling between dimerization and ubiquitin binding. J Mol Biol (2009) 1.02

Nicotine enhances intracellular nicotinic receptor maturation: a novel mechanism of neural plasticity? J Physiol Paris (2006) 1.01

Nicotinic receptors regulate the survival of newborn neurons in the adult olfactory bulb. Proc Natl Acad Sci U S A (2004) 1.01