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Binding of a negative allosteric modulator and competitive antagonist can occur simultaneously at the ionotropic glutamate receptor GluA2

The FEBS journal, 2021-02, Vol.288 (3), p.995-1007

2021

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7‑Phenoxy-Substituted 3,4-Dihydro‑2H‑1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of α‑Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency

Journal of medicinal chemistry, 2018-01, Vol.61 (1), p.251-264

2018

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Exploring thienothiadiazine dioxides as isosteric analogues of benzo- and pyridothiadiazine dioxides in the search of new AMPA and kainate receptor positive allosteric modulators

European journal of medicinal chemistry, 2024-01, Vol.264, p.116036-116036, Article 116036

2024

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Neuroplastin-55 binds to and signals through the fibroblast growth factor receptor

The FASEB journal, 2010-04, Vol.24 (4), p.1139-1150

2010

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Small-angle neutron scattering studies on the AMPA receptor GluA2 in the resting, AMPA-bound and GYKI-53655-bound states

IUCrJ, 2018-11, Vol.5 (Pt 6), p.780-793

2018

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Structural basis for positive allosteric modulation of AMPA and kainate receptors

The Journal of physiology, 2022-01, Vol.600 (2), p.181-200

2022

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Recovery from desensitization in GluA2 AMPA receptors is affected by a single mutation in the N-terminal domain interface

The Journal of biological chemistry, 2024-03, Vol.300 (3), p.105717-105717, Article 105717

2024

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Enhancing Action of Positive Allosteric Modulators through the Design of Dimeric Compounds

Journal of medicinal chemistry, 2018-06, Vol.61 (12), p.5279-5291

2018

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The positive allosteric modulator BPAM344 and L‐glutamate introduce an active‐like structure of the ligand‐binding domain of GluK2

FEBS letters, 2024-04, Vol.598 (7), p.743-757

2024

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Differences between the GluD1 and GluD2 receptors revealed by GluD1 X‐ray crystallography, binding studies and molecular dynamics

The FEBS journal, 2023-08, Vol.290 (15), p.3781-3801

2023

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Crystal structure of the GluK1 ligand-binding domain with kainate and the full-spanning positive allosteric modulator BPAM538

Journal of structural biology, 2024-09, Vol.216 (3), p.108113, Article 108113

2024

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Lessons from more than 80 structures of the GluA2 ligand-binding domain in complex with agonists, antagonists and allosteric modulators

Neuropharmacology, 2011, Vol.60 (1), p.135-150

2011

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Identification and Structure-Function Study of Positive Allosteric Modulators of Kainate Receptors

Molecular pharmacology, 2017-06, Vol.91 (6), p.576-585

2017

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Partial Agonism and Antagonism of the Ionotropic Glutamate Receptor iGLuR5

The Journal of biological chemistry, 2007-08, Vol.282 (35), p.25726-25736

2007

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A pharmacological profile of the high-affinity GluK5 kainate receptor

European journal of pharmacology, 2016-10, Vol.788, p.315-320

2016

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The low binding affinity of D-serine at the ionotropic glutamate receptor GluD2 can be attributed to the hinge region

Scientific reports, 2017-04, Vol.7 (1), p.46145-46145, Article 46145

2017

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Development of Thiochroman Dioxide Analogues of Benzothiadiazine Dioxides as New Positive Allosteric Modulators of α‑Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors

ACS chemical neuroscience, 2021-07, Vol.12 (14), p.2679-2692

2021

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(S)‑2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements and Structural and Biological Investigation

Journal of medicinal chemistry, 2018-03, Vol.61 (5), p.2124-2130

2018

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Crystal Structures of Potent Dimeric Positive Allosteric Modulators at the Ligand-Binding Domain of the GluA2 Receptor

ACS medicinal chemistry letters, 2019-03, Vol.10 (3), p.243-247

2019

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Intersubunit bridge formation governs agonist efficacy at nicotinic acetylcholine α4β2 receptors: unique role of halogen bonding revealed

The Journal of biological chemistry, 2012-02, Vol.287 (6), p.4248-4259

2012

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The ionotropic glutamate receptor GluA2 in complex with bicyclic pyrimidinedione-based compounds: when small compound modifications have distinct effects on binding interactions

ACS chemical neuroscience, 2020-06, Vol.11 (12), p.1791-1800

2020

Volltextzugriff (PDF)

7-Phenoxy-Substituted 3,4-Dihydro-2 H -1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency

Journal of medicinal chemistry, 2018-01, Vol.61 (1), p.251-264

2018

Volltextzugriff (PDF)

N 1-Substituted Quinoxaline-2,3-diones as Kainate Receptor Antagonists: X-ray Crystallography, Structure–Affinity Relationships, and in Vitro Pharmacology

ACS chemical neuroscience, 2019-03, Vol.10 (3), p.1841-1853

2019

Volltextzugriff (PDF)

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

The Journal of biological chemistry, 2013-11, Vol.288 (46), p.33124-33135

2013

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Binding of a negative allosteric modulator and competitive antagonist can occur simultaneously at the ionotropic glutamate receptor GluA2

7‑Phenoxy-Substituted 3,4-Dihydro‑2H‑1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of α‑Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency

Exploring thienothiadiazine dioxides as isosteric analogues of benzo- and pyridothiadiazine dioxides in the search of new AMPA and kainate receptor positive allosteric modulators

Neuroplastin-55 binds to and signals through the fibroblast growth factor receptor

Small-angle neutron scattering studies on the AMPA receptor GluA2 in the resting, AMPA-bound and GYKI-53655-bound states

Structural basis for positive allosteric modulation of AMPA and kainate receptors

Recovery from desensitization in GluA2 AMPA receptors is affected by a single mutation in the N-terminal domain interface

Enhancing Action of Positive Allosteric Modulators through the Design of Dimeric Compounds

The positive allosteric modulator BPAM344 and L‐glutamate introduce an active‐like structure of the ligand‐binding domain of GluK2

Differences between the GluD1 and GluD2 receptors revealed by GluD1 X‐ray crystallography, binding studies and molecular dynamics

Crystal structure of the GluK1 ligand-binding domain with kainate and the full-spanning positive allosteric modulator BPAM538

Lessons from more than 80 structures of the GluA2 ligand-binding domain in complex with agonists, antagonists and allosteric modulators

Identification and Structure-Function Study of Positive Allosteric Modulators of Kainate Receptors

Partial Agonism and Antagonism of the Ionotropic Glutamate Receptor iGLuR5

A pharmacological profile of the high-affinity GluK5 kainate receptor

The low binding affinity of D-serine at the ionotropic glutamate receptor GluD2 can be attributed to the hinge region

Invisible detergents for structure determination of membrane proteins by small‐angle neutron scattering

Development of Thiochroman Dioxide Analogues of Benzothiadiazine Dioxides as New Positive Allosteric Modulators of α‑Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors

(S)‑2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements and Structural and Biological Investigation

Crystal Structures of Potent Dimeric Positive Allosteric Modulators at the Ligand-Binding Domain of the GluA2 Receptor

Intersubunit bridge formation governs agonist efficacy at nicotinic acetylcholine α4β2 receptors: unique role of halogen bonding revealed

The ionotropic glutamate receptor GluA2 in complex with bicyclic pyrimidinedione-based compounds: when small compound modifications have distinct effects on binding interactions

7-Phenoxy-Substituted 3,4-Dihydro-2 H -1,2,4-benzothiadiazine 1,1-Dioxides as Positive Allosteric Modulators of α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptors with Nanomolar Potency

N 1-Substituted Quinoxaline-2,3-diones as Kainate Receptor Antagonists: X-ray Crystallography, Structure–Affinity Relationships, and in Vitro Pharmacology

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

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