List of works - Margot Ernst

A novel GABA(A) receptor pharmacology: drugs interacting with the α(+) β(-) interface

scientific article published on May 2012

A novel de novo variant of GABRA1 causes increased sensitivity for GABA in vitro

scientific article published on 11 February 2020

A pentasymmetric open channel blocker for Cys-loop receptor channels

scientific article

Accelerated discovery of novel benzodiazepine ligands by experiment-guided virtual screening.

scientific article

Allosteric GABAA Receptor Modulators-A Review on the Most Recent Heterocyclic Chemotypes and Their Synthetic Accessibility

scientific article published on 24 February 2020

An updated unified pharmacophore model of the benzodiazepine binding site on gamma-aminobutyric acid(a) receptors: correlation with comparative models

scientific article

Attaining in vivo selectivity of positive modulation of α3βγ2 GABAA receptors in rats: A hard task!

scientific article published on 19 June 2018

Cerebellar α6 subunit-containing GABAA receptors: A novel therapeutic target for disrupted prepulse inhibition in neuropsychiatric disorders.

scientific article published on 8 March 2018

Comparative modeling of GABA(A) receptors: limits, insights, future developments.

scientific article

Comparative models of GABAA receptor extracellular and transmembrane domains: important insights in pharmacology and function.

scientific article

Corrigendum to "Metal-assisted synthesis of unsymmetrical magnolol and honokiol analogs and their biological assessment as GABAA receptor ligands" [Bioorg. Med. Chem. Lett. 25/2 (2015) 400-403].

scientific article published on 20 February 2015

Defined concatenated α6α1β3γ2 GABAA receptor constructs reveal dual action of pyrazoloquinolinone allosteric modulators

scientific article published on 05 June 2019

Design and Synthesis of Novel Deuterated Ligands Functionally Selective for the γ-Aminobutyric Acid Type A Receptor (GABAAR) α6 Subtype with Improved Metabolic Stability and Enhanced Bioavailability.

scientific article published on 26 February 2018

Development of GABAA Receptor Subtype-Selective Imidazobenzodiazepines as Novel Asthma Treatments

scientific article published on 27 April 2016

Diazepam-bound GABAA receptor models identify new benzodiazepine binding-site ligands

scientific article

Different Benzodiazepines Bind with Distinct Binding Modes to GABAA Receptors

scientific article published on 23 July 2018

Diversity matters: combinatorial information coding by GABAA receptor subunits during spatial learning and its allosteric modulation

scientific article published on 11 July 2018

Engineered Flumazenil Recognition Site Provides Mechanistic Insight Governing Benzodiazepine Modulation in GABA Receptors

scientific article published on 23 July 2018

Ester to amide substitution improves selectivity, efficacy and kinetic behavior of a benzodiazepine positive modulator of GABAA receptors containing the α5 subunit

scientific article

Expeditious synthesis of polyacetylenic water hemlock toxins and their effects on the major GABAA receptor isoform.

scientific article published on 7 February 2018

First In Vivo Testing of Compounds Targeting Group 3 Medulloblastomas Using an Implantable Microdevice as a New Paradigm for Drug Development.

scientific article

GABAA Receptor Ligands Often Interact with Binding Sites in the Transmembrane Domain and in the Extracellular Domain-Can the Promiscuity Code Be Cracked?

scientific article published on 03 January 2020

Heterogeneity of GABAA Receptors: Revived Interest in the Development of Subtype-selective Drugs

article

Identification of amino acid residues important for assembly of GABA receptor alpha1 and gamma2 subunits.

scientific article published on 12 January 2006

Identification of novel positive allosteric modulators and null modulators at the GABAA receptor α+β- interface

scientific article published on May 2013

Identification of the putative binding pocket of valerenic acid on GABAA receptors using docking studies and site-directed mutagenesis.

scientific article published on 16 September 2015

Metal-assisted synthesis of unsymmetrical magnolol and honokiol analogs and their biological assessment as GABAA receptor ligands

scientific article

Molecular analysis of the site for 2-arachidonylglycerol (2-AG) on the β₂ subunit of GABA(A) receptors

scientific article

Molecular basis of mood and cognitive adverse events elucidated via a combination of pharmacovigilance data mining and functional enrichment analysis

scientific article published on 05 June 2020

Molecular tools for GABAA receptors: High affinity ligands for β1-containing subtypes.

scientific article

Mutagenesis and computational docking studies support the existence of a histamine binding site at the extracellular β3+β3- interface of homooligomeric β3 GABAA receptors

scientific article published on 29 April 2016

Negative allosteric modulation of alpha 5-containing GABAA receptors engenders antidepressant-like effects and selectively prevents age-associated hyperactivity in tau-depositing mice

scientific article published on 26 January 2018

Pentameric ligand-gated ion channel ELIC is activated by GABA and modulated by benzodiazepines

scientific article

Pharmacological and antihyperalgesic properties of the novel α2/3 preferring GABAA receptor ligand MP-III-024.

scientific article published on 4 March 2017

Proximity-accelerated chemical coupling reaction in the benzodiazepine-binding site of gamma-aminobutyric acid type A receptors: superposition of different allosteric modulators.

scientific article published on 11 July 2007

SAR-Guided Scoring Function and Mutational Validation Reveal the Binding Mode of CGS-8216 at the α1+/γ2– Benzodiazepine Site

scientific article published on 08 August 2018

Spontaneous cross-link of mutated alpha1 subunits during GABA(A) receptor assembly.

scientific article published on 4 December 2006

Structural Studies of GABAA Receptor Binding Sites: Which Experimental Structure Tells us What?

scientific article published on 16 June 2016

Subtype selectivity of α+β- site ligands of GABAA receptors: identification of the first highly specific positive modulators at α6β2/3γ2 receptors.

scientific article published on May 2013

Synthesis and Characterization of a Novel γ-Aminobutyric Acid Type A (GABAA) Receptor Ligand That Combines Outstanding Metabolic Stability, Pharmacokinetics, and Anxiolytic Efficacy

scientific article published on 28 November 2016

Targeting the γ-Aminobutyric Acid A Receptor α4 Subunit in Airway Smooth Muscle to Alleviate Bronchoconstriction.

scientific article published on 25 September 2015

The Benzodiazepine Binding Sites of GABAA Receptors

scientific article

The GABAA receptor alpha+beta- interface: a novel target for subtype selective drugs

scientific article

The α6 subunit-containing GABA receptor: A novel drug target for inhibition of trigeminal activation

scholarly article by Pi-Chuan Fan et al published 15 September 2018 in Neuropharmacology

Towards functional selectivity for α6β3γ2 GABAA receptors: a series of novel pyrazoloquinolinones.

scientific article published on 11 November 2017

Trigeminal neuropathic pain development and maintenance in rats are suppressed by a positive modulator of α6 GABAA receptors

scientific article published on 04 February 2019

Understanding subtype-selective allosteric modulation of GABAA receptors.

scientific article published on 17 September 2012

Unexpected Properties of δ-Containing GABAA Receptors in Response to Ligands Interacting with the α+ β- Site.

scientific article published on 26 September 2013

Variations on a scaffold - Novel GABAA receptor modulators

scientific article published on 05 July 2019

α subunits in GABAA receptors are dispensable for GABA and diazepam action.

scientific article published on 14 November 2017

List of works by Margot Ernst

A novel GABA(A) receptor pharmacology: drugs interacting with the α(+) β(-) interface

A novel de novo variant of GABRA1 causes increased sensitivity for GABA in vitro

A pentasymmetric open channel blocker for Cys-loop receptor channels

Accelerated discovery of novel benzodiazepine ligands by experiment-guided virtual screening.

Allosteric GABAA Receptor Modulators-A Review on the Most Recent Heterocyclic Chemotypes and Their Synthetic Accessibility

An updated unified pharmacophore model of the benzodiazepine binding site on gamma-aminobutyric acid(a) receptors: correlation with comparative models

Attaining in vivo selectivity of positive modulation of α3βγ2 GABAA receptors in rats: A hard task!

Cerebellar α6 subunit-containing GABAA receptors: A novel therapeutic target for disrupted prepulse inhibition in neuropsychiatric disorders.

Comparative modeling of GABA(A) receptors: limits, insights, future developments.

Comparative models of GABAA receptor extracellular and transmembrane domains: important insights in pharmacology and function.

Corrigendum to "Metal-assisted synthesis of unsymmetrical magnolol and honokiol analogs and their biological assessment as GABAA receptor ligands" [Bioorg. Med. Chem. Lett. 25/2 (2015) 400-403].

Defined concatenated α6α1β3γ2 GABAA receptor constructs reveal dual action of pyrazoloquinolinone allosteric modulators

Design and Synthesis of Novel Deuterated Ligands Functionally Selective for the γ-Aminobutyric Acid Type A Receptor (GABAAR) α6 Subtype with Improved Metabolic Stability and Enhanced Bioavailability.

Development of GABAA Receptor Subtype-Selective Imidazobenzodiazepines as Novel Asthma Treatments

Diazepam-bound GABAA receptor models identify new benzodiazepine binding-site ligands

Different Benzodiazepines Bind with Distinct Binding Modes to GABAA Receptors

Diversity matters: combinatorial information coding by GABAA receptor subunits during spatial learning and its allosteric modulation

Engineered Flumazenil Recognition Site Provides Mechanistic Insight Governing Benzodiazepine Modulation in GABA Receptors

Ester to amide substitution improves selectivity, efficacy and kinetic behavior of a benzodiazepine positive modulator of GABAA receptors containing the α5 subunit

Expeditious synthesis of polyacetylenic water hemlock toxins and their effects on the major GABAA receptor isoform.

First In Vivo Testing of Compounds Targeting Group 3 Medulloblastomas Using an Implantable Microdevice as a New Paradigm for Drug Development.

GABAA Receptor Ligands Often Interact with Binding Sites in the Transmembrane Domain and in the Extracellular Domain-Can the Promiscuity Code Be Cracked?

Heterogeneity of GABAA Receptors: Revived Interest in the Development of Subtype-selective Drugs

Identification of amino acid residues important for assembly of GABA receptor alpha1 and gamma2 subunits.

Identification of novel positive allosteric modulators and null modulators at the GABAA receptor α+β- interface

Identification of the putative binding pocket of valerenic acid on GABAA receptors using docking studies and site-directed mutagenesis.

Metal-assisted synthesis of unsymmetrical magnolol and honokiol analogs and their biological assessment as GABAA receptor ligands

Molecular analysis of the site for 2-arachidonylglycerol (2-AG) on the β₂ subunit of GABA(A) receptors

Molecular basis of mood and cognitive adverse events elucidated via a combination of pharmacovigilance data mining and functional enrichment analysis

Molecular tools for GABAA receptors: High affinity ligands for β1-containing subtypes.

Mutagenesis and computational docking studies support the existence of a histamine binding site at the extracellular β3+β3- interface of homooligomeric β3 GABAA receptors

Negative allosteric modulation of alpha 5-containing GABAA receptors engenders antidepressant-like effects and selectively prevents age-associated hyperactivity in tau-depositing mice

Pentameric ligand-gated ion channel ELIC is activated by GABA and modulated by benzodiazepines

Pharmacological and antihyperalgesic properties of the novel α2/3 preferring GABAA receptor ligand MP-III-024.

Proximity-accelerated chemical coupling reaction in the benzodiazepine-binding site of gamma-aminobutyric acid type A receptors: superposition of different allosteric modulators.

SAR-Guided Scoring Function and Mutational Validation Reveal the Binding Mode of CGS-8216 at the α1+/γ2– Benzodiazepine Site

Spontaneous cross-link of mutated alpha1 subunits during GABA(A) receptor assembly.

Structural Studies of GABAA Receptor Binding Sites: Which Experimental Structure Tells us What?

Subtype selectivity of α+β- site ligands of GABAA receptors: identification of the first highly specific positive modulators at α6β2/3γ2 receptors.

Synthesis and Characterization of a Novel γ-Aminobutyric Acid Type A (GABAA) Receptor Ligand That Combines Outstanding Metabolic Stability, Pharmacokinetics, and Anxiolytic Efficacy

Targeting the γ-Aminobutyric Acid A Receptor α4 Subunit in Airway Smooth Muscle to Alleviate Bronchoconstriction.

The Benzodiazepine Binding Sites of GABAA Receptors

The GABAA receptor alpha+beta- interface: a novel target for subtype selective drugs

The α6 subunit-containing GABA receptor: A novel drug target for inhibition of trigeminal activation

Towards functional selectivity for α6β3γ2 GABAA receptors: a series of novel pyrazoloquinolinones.

Trigeminal neuropathic pain development and maintenance in rats are suppressed by a positive modulator of α6 GABAA receptors

Understanding subtype-selective allosteric modulation of GABAA receptors.

Unexpected Properties of δ-Containing GABAA Receptors in Response to Ligands Interacting with the α+ β- Site.

Variations on a scaffold - Novel GABAA receptor modulators

α subunits in GABAA receptors are dispensable for GABA and diazepam action.