The structure of a mixed GluR2 ligand-binding core dimer in complex with (S)-glutamate and the antagonist (S)-NS1209.

No abstract is available for this paper.

• Publication year

  2006

• Venue

  Journal of Molecular Biology

• Publication date

  2006-04-07

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1016/J.JMB.2006.01.024PMID 16483599
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Tyr702 Is an Important Determinant of Agonist Binding and Domain Closure of the Ligand-Binding Core of GluR2

  2005cited by this paper
• A Binding Site Tyrosine Shapes Desensitization Kinetics and Agonist Potency at GluR2

  2005cited by this paper
• Structure of the kainate receptor subunit GluR6 agonist-binding domain complexed with domoic acid.

  2005cited by this paper
• Subunit arrangement and function in NMDA receptors

  2005cited by this paper
• Exploring the GluR2 ligand‐binding core in complex with the bicyclical AMPA analogue (S)‐4‐AHCP

  2005cited by this paper
• Structural determinants of agonist-specific kinetics at the ionotropic glutamate receptor 2.

  2005cited by this paper
• Crystal structures of the GluR5 and GluR6 ligand binding cores: molecular mechanisms underlying kainate receptor selectivity.

  2005cited by this paper
• Crystal structure of the kainate receptor GluR5 ligand‐binding core in complex with (S)‐glutamate

  2005cited by this paper
• Regulation of AMPA receptor gating by ligand binding core dimers.

  2004cited by this paper
• How AMPA Receptor Desensitization Depends on Receptor Occupancy

  2003cited by this paper
• Structural basis for partial agonist action at ionotropic glutamate receptors

  2003cited by this paper
• Three-dimensional structure of the ligand-binding core of GluR2 in complex with the agonist (S)-ATPA: implications for receptor subunit selectivity.

  2003cited by this paper
• Mechanisms of activation, inhibition and specificity: crystal structures of the NMDA receptor NR1 ligand‐binding core

  2003cited by this paper
• Competitive antagonism of AMPA receptors by ligands of different classes: crystal structure of ATPO bound to the GluR2 ligand-binding core, in comparison with DNQX.

  2003cited by this paper
• Design, synthesis, and pharmacology of a highly subtype-selective GluR1/2 agonist, (RS)-2-amino-3-(4-chloro-3-hydroxy-5-isoxazolyl)propionic acid (Cl-HIBO).

  2003cited by this paper
• Probing the function, conformational plasticity, and dimer-dimer contacts of the GluR2 ligand-binding core: studies of 5-substituted willardiines and GluR2 S1S2 in the crystal.

  2003cited by this paper
• GluR2 ligand‐binding core complexes: importance of the isoxazolol moiety and 5‐substituent for the binding mode of AMPA‐type agonists

  2002cited by this paper
• Structural basis for AMPA receptor activation and ligand selectivity: crystal structures of five agonist complexes with the GluR2 ligand-binding core.

  2002cited by this paper
• Mechanism of activation and selectivity in a ligand-gated ion channel: structural and functional studies of GluR2 and quisqualate.

  2002cited by this paper
• Correlation between Anticonvulsant Activity and Inhibitory Action on Glial γ-Aminobutyric Acid Uptake of the Highly Selective Mouse γ-Aminobutyric Acid Transporter 1 Inhibitor 3-Hydroxy-4-amino-4,5,6,7-tetrahydro-1,2-benzisoxazole and ItsN-Alkylated Analogs

  2002cited by this paper
• Mechanism of glutamate receptor desensitization

  2002cited by this paper
• Ion channel structure: The structure and function of glutamate receptor ion channels

  2002cited by this paper
• Identification of Amino Acid Residues in GluR1 Responsible for Ligand Binding and Desensitization

  2001cited by this paper
• Domain Interactions Regulating AMPA Receptor Desensitization

  2001cited by this paper
• Mechanisms for ligand binding to GluR0 ion channels: crystal structures of the glutamate and serine complexes and a closed apo state.

  2001cited by this paper
• Ligands for glutamate receptors: design and therapeutic prospects.

  2000cited by this paper
• Large-scale expression and thermodynamic characterization of a glutamate receptor agonist-binding domain.

  2000cited by this paper
• Mechanisms for activation and antagonism of an AMPA-sensitive glutamate receptor: crystal structures of the GluR2 ligand binding core.

  2000cited by this paper
• Exact analysis of competition ligand binding by displacement isothermal titration calorimetry.

  2000cited by this paper
• Agonist discrimination between AMPA receptor subtypes

  2000cited by this paper
• Further additions to MolScript version 1.4, including reading and contouring of electron-density maps.

  1999cited by this paper
• SPD 502: a water-soluble and in vivo long-lasting AMPA antagonist with neuroprotective activity.

  1999cited by this paper
• The glutamate receptor ion channels.

  1999cited by this paper
• Crystallography & NMR system: A new software suite for macromolecular structure determination.

  1998cited by this paper
• Structure of a glutamate-receptor ligand-binding core in complex with kainate

  1998cited by this paper
• Pharmacological properties of homomeric and heteromeric GluR1o and GluR3o receptors.

  1998cited by this paper
• A point mutation in the glutamate binding site blocks desensitization of AMPA receptors.

  1998cited by this paper
• Probing the ligand binding domain of the GluR2 receptor by proteolysis and deletion mutagenesis defines domain boundaries and yields a crystallizable construct

  1998cited by this paper
• Evidence for a Tetrameric Structure of Recombinant NMDA Receptors

  1998cited by this paper
• The tetrameric structure of a glutamate receptor channel.

  1998cited by this paper
• Glutamate in CNS disorders as a target for drug development: an update.

  1998cited by this paper
• Protein domain movements: detection of rigid domains and visualization of hinges in comparisons of atomic coordinates

  1997cited by this paper
• Processing of X-ray diffraction data collected in oscillation mode.

  1997cited by this paper
• [20] Processing of X-ray diffraction data collected in oscillation mode.

  1997cited by this paper
• Stable expression of homomeric AMPA-selective glutamate receptors in BHK cells.

  1996cited by this paper
• Phi/psi-chology: Ramachandran revisited.

  1996cited by this paper
• VMD: visual molecular dynamics.

  1996cited by this paper
• Molecular dissection of the agonist binding site of an AMPA receptor.

  1995cited by this paper
• Raster3D Version 2.0. A program for photorealistic molecular graphics.

  1994cited by this paper
• The CCP4 suite: programs for protein crystallography.

  1994cited by this paper
• AMoRe: an automated package for molecular replacement

  1994cited by this paper
• A program to produce both detailed and schematic plots of protein structures

  1991cited by this paper
• Improved methods for building protein models in electron density maps and the location of errors in these models.

  1991cited by this paper
• Rapid measurement of binding constants and heats of binding using a new titration calorimeter.

  1989cited by this paper
• Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.

  1973cited by this paper

• Biological properties of pyrroloquinoline and pyrroloisoquinoline derivatives.

  2024cites this paper
• Kainate Receptor Antagonists: Recent Advances and Therapeutic Perspective

  2023cites this paper
• Structure, Function, and Pharmacology of Glutamate Receptor Ion Channels

  2021cites this paper
• Computational Investigation into the Interactions of Traditional Chinese Medicine Molecules of WenQingYin with GluR2

  2017cites this paper
• NS1209/SPD 502, A Novel Selective AMPA Antagonist for Stroke, Neuropathic Pain or Epilepsy? Drug Development Lessons Learned

  2017cites this paper
• A parallel panning scheme used for selection of a GluA4-specific Fab targeting the ligand-binding domain.

  2016cites this paper
• Studies on Aryl-Substituted Phenylalanines: Synthesis, Activity, and Different Binding Modes at AMPA Receptors.

  2016cites this paper
• Pharmacology and Structural Analysis of Ligand Binding to the Orthosteric Site of Glutamate-Like GluD2 Receptors

  2016influential citation
• Binding mode of an α-amino acid-linked quinoxaline-2,3-dione analogue at glutamate receptor subtype GluK1.

  2015cites this paper
• GluD2: GluD2 receptors containing the lurcher mutation iGluRs: Ionotropic glutamate receptors ITC: Isothermal titration calorimetry LBD: Ligand binding domain LTP: Long-term potentiation LTD: Long-term depression NMDA: N-methyl-D-aspartate NMDAR: NMDA receptor PSD: Postsynaptic density SAR: Structur

  2015influential citation
• Proteins and azobenzenes

  2013cites this paper
• Molecular Mechanism of a Novel GluN 1 Glycine-Site Antagonist ! " ! ! Crystal Structure and Pharmacological Characterization of a Novel NMDA Receptor Antagonist at the GluN 1 Glycine Binding Site

  2013cites this paper
• Heterocycles as Nonclassical Bioisosteres of α‐Amino Acids

  2013cites this paper
• Studies on an (S)-2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptor antagonist IKM-159: asymmetric synthesis, neuroactivity, and structural characterization.

  2013cites this paper
• Crystal Structure and Pharmacological Characterization of a Novel N-Methyl-d-aspartate (NMDA) Receptor Antagonist at the GluN1 Glycine Binding Site*

  2013cites this paper
• Structure-based discovery of antagonists for GluN3-containing N-methyl-D-aspartate receptors.

  2013cites this paper
• Investigating Drug Interactions: From Thermodynamic Driving Forces Of Ligand Binding To In Vivo Multiphoton Microscopy Of Chemotherapy Drug Intrinsic Fluorescence

  2013cites this paper
• New AMPA antagonists in epilepsy

  2012cites this paper
• The Structure of (−)-Kaitocephalin Bound to the Ligand Binding Domain of the (S)-α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA)/Glutamate Receptor, GluA2*

  2012cites this paper
• Glutamatergic neurotransmission as molecular target of new anticonvulsants.

  2012cites this paper
• Size matters in activation/inhibition of ligand-gated ion channels.

  2012cites this paper
• Ionotropic Glutamate Receptors (iGluRs): Overview of iGluR2 ligand binding domain in complex with agonists and antagonists

  2011influential citation
• Molecular targets for antiepileptic drug development

  2011cites this paper
• A new phenylalanine derivative acts as an antagonist at the AMPA receptor GluA2 and introduces partial domain closure: synthesis, resolution, pharmacology, and crystal structure.

  2011cites this paper
• Lessons from more than 80 structures of the GluA2 ligand-binding domain in complex with agonists, antagonists and allosteric modulators.

  2011cites this paper
• Binding site and ligand flexibility revealed by high resolution crystal structures of GluK1 competitive antagonists.

  2011influential citation
• Quantifying Water-Mediated Protein–Ligand Interactions in a Glutamate Receptor: A DFT Study

  2011cites this paper
• Medicinal chemistry of competitive kainate receptor antagonists.

  2011cites this paper
• Glutamate Receptor Ion Channels: Structure, Regulation, and Function

  2010cites this paper
• Pharmacology of ionotropic glutamate receptors: A structural perspective.

  2010cites this paper
• Molecular structure of ionotropic glutamate receptors.

  2010cites this paper
• Hydrophobic Side Chain Dynamics of a Glutamate Receptor Ligand Binding Domain*

  2010cites this paper
• Single-molecule FRET Analysis of the Dynamics of AMP A Receptor

  2010cites this paper
• Ion channel blockers for the treatment of neuropathic pain.

  2010cites this paper
• Energy transfer ligands of the GluR2 ligand binding core.

  2010cites this paper
• Thermodynamics of Peptide and Non-Peptide Interactions with the Human 5HT1a Receptor

  2010cites this paper
• Mechanisms of antagonism of the GluR2 AMPA receptor: structure and dynamics of the complex of two willardiine antagonists with the glutamate binding domain.

  2009influential citation
• Kainate receptors: pharmacology, function and therapeutic potential.

  2009cites this paper
• AMPA Receptor Ligand Binding Domain Mobility Revealed by Functional Cross Linking

  2009cites this paper
• Structures of the ligand-binding core of iGluR2 in complex with the agonists (R)- and (S)-2-amino-3-(4-hydroxy-1,2,5-thiadiazol-3-yl)propionic acid explain their unusual equipotency.

  2008cites this paper
• Interplay between structural rigidity and electrostatic interactions in the ligand binding domain of GluR2

  2008cites this paper
• A survey of the year 2006 literature on applications of isothermal titration calorimetry

  2008cites this paper
• Structural Correlates of Ionotropic Glutamate Receptor Function

  2008cites this paper
• Year : 2008 A survey of the year 2006 literature on applications of isothermal titration calorimetry

  2008cites this paper
• Partial Agonism and Antagonism of the Ionotropic Glutamate Receptor iGLuR5

  2007cites this paper
• Structural aspects of AMPA receptor activation, desensitization and deactivation.

  2007cites this paper
• Dynamics of the S1S2 Glutamate Binding Domain of GluR2 Measured Using 19F NMR Spectroscopy*

  2007cites this paper
• Survey of the year 2005: literature on applications of isothermal titration calorimetry

  2007cites this paper
• Flexibility of a glutamate-binding domain.

  2007cites this paper
• Two conformational changes are associated with glutamate translocation by the glutamate transporter EAAC1.

  2007cites this paper
• Structural proof of a dimeric positive modulator bridging two identical AMPA receptor-binding sites.

  2007cites this paper
• Progress report on new antiepileptic drugs: a summary of the Eigth Eilat Conference (EILAT VIII).

  2007cites this paper
• Glutamate receptor ion channels.

  2005cites this paper