List of works - Leggy A Arnold

A Novel Orally Available Asthma Drug Candidate That Reduces Smooth Muscle Constriction and Inflammation by Targeting GABAA Receptors in the Lung.

scientific article published on 26 March 2018

A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model

scientific article

A Structure-Activity Relationship Comparison of Imidazodiazepines Binding at Kappa, Mu, and Delta Opioid Receptors and the GABAA Receptor

scientific article published on 25 August 2020

A fluorescence-based high throughput assay for the determination of small molecule-human serum albumin protein binding

scientific article

A high-throughput ligand competition binding assay for the androgen receptor and other nuclear receptors.

scientific article published on January 2009

A high-throughput screening assay for pyruvate carboxylase.

scientific article published on 12 April 2018

A high-throughput screening method to identify small molecule inhibitors of thyroid hormone receptor coactivator binding

scientific article published on 27 June 2006

A new catalytic and enantioselective desymmetrization of symmetrical methylidene cycloalkene oxides

scientific article published on 01 April 2000

A novel GABAA receptor ligand MIDD0301 with limited blood-brain barrier penetration relaxes airway smooth muscle ex vivo and in vivo

scientific article published on 29 November 2018

A quantitative high-throughput screen identifies novel inhibitors of the interaction of thyroid receptor beta with a peptide of steroid receptor coactivator 2

scientific article

A surface on the androgen receptor that allosterically regulates coactivator binding

scientific article

Alleviation of Multiple Asthmatic Pathologic Features with Orally Available and Subtype Selective GABAA Receptor Modulators

scientific article published on 25 April 2017

Alternative binding sites at the vitamin D receptor and their ligands

scientific article published on 14 January 2019

An anthrone-based Kv7.2/7.3 channel blocker with improved properties for the investigation of psychiatric and neurodegenerative disorders

scientific article published on 14 September 2019

An integrated in vitro and in vivo high-throughput screen identifies treatment leads for ependymoma.

scientific article

Anticancer activity of VDR-coregulator inhibitor PS121912.

scientific article

Antitumor Activity of 3-Indolylmethanamines 31B and PS121912.

scientific article

Calcitroic Acid-A Review.

scientific article

Catalytic enantioselective synthesis of (-)-prostaglandin E1 methyl ester based on a tandem 1,4-addition-aldol reaction

scientific article published in October 2002

Characterization of GABAA receptor ligands with automated patch-clamp using human neurons derived from pluripotent stem cells

scientific article published on 17 August 2016

Comparison of cell expression formats for the characterization of GABA(A) channels using a microfluidic patch clamp system

scientific article

Copper phosphoramidite catalyzed enantioselective ring-opening of oxabicyclic alkenes: remarkable reversal of stereocontrol.

scientific article

Correction to "A Novel Orally Available Asthma Drug Candidate That Reduces Smooth Muscle Constriction and Inflammation by Targeting GABAA Receptors in the Lung"

scientific article published on 21 October 2019

Design and Evaluation of Heterobivalent PAR1-PAR2 Ligands as Antagonists of Calcium Mobilization

scientific article published on 03 December 2018

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

Development of novel Vitamin D Receptor-Coactivator Inhibitors

scientific article published on February 2014

Differential regulation of epidermal function by VDR coactivators

scientific article

Discovery and Optimization of Novel Hydrogen Peroxide Activated Aromatic Nitrogen Mustard Derivatives as Highly Potent Anticancer Agents

scientific article published on 10 October 2018

Discovery of small molecule inhibitors of the interaction of the thyroid hormone receptor with transcriptional coregulators

scientific article published on 31 October 2005

Discovery of the first irreversible small molecule inhibitors of the interaction between the vitamin D receptor and coactivators

scientific article published on 16 May 2012

Efficacy of a non-hypercalcemic vitamin-D2 derived anti-cancer agent (MT19c) and inhibition of fatty acid synthesis in an ovarian cancer xenograft model

scientific article

Enantioselective copper-catalyzed allylic alkylation with dialkylzincs using phosphoramidite ligands

scientific article published on 01 April 2001

Evaluation of the first Ergocalciferol-derived, non hypercalcemic anti-cancer agent MT19c in ovarian cancer SKOV-3 cell lines ⬇️

scientific article published on July 30, 2011

Further evaluation of the potential anxiolytic activity of imidazo[1,5-a][1,4]diazepin agents selective for α2/3-containing GABAA receptors

scientific article published on 22 April 2017

Genetic and pharmacological manipulation of glyoxalase 1 regulates voluntary ethanol consumption in mice

scientific article published on 22 December 2015

Glo1 inhibitors for neuropsychiatric and anti-epileptic drug development

scientific article

High-throughput identification of promiscuous inhibitors from screening libraries with the use of a thiol-containing fluorescent probe

scientific article

Highly Enantioselective Copper-Phosphoramidite Catalyzed Kinetic Resolution of Chiral 2-Cyclohexenones

scientific article published in March 2001

Highly Enantioselective Copper-Phosphoramidite Catalyzed Kinetic Resolution of Chiral 2-Cyclohexenones This work was supported by the Dutch Foundation for Scientific Research (NWO)

scientific article published on 01 March 2001

Hydrogen peroxide activated quinone methide precursors with enhanced DNA cross-linking capability and cytotoxicity towards cancer cells.

scientific article published on 24 March 2017

IDENTIFICATION OF VDR ANTAGONISTS AMONG NUCLEAR RECEPTOR LIGANDS USING VIRTUAL SCREENING

scientific article published on January 2014

Identification and analysis of hepatitis C virus NS3 helicase inhibitors using nucleic acid binding assays

scientific article

Identification and characterization of the first small molecule inhibitor of MDMX

scientific article

Identification of a Vitamin-D Receptor Antagonist, MeTC7, which Inhibits the Growth of Xenograft and Transgenic Tumors <i>In Vivo</i>

scientific article published on 11 April 2022

Identification of a novel, fast-acting GABAergic antidepressant

scientific article published on 21 March 2017

Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors.

scientific article published on July 2009

Inhibition of a viral enzyme by a small-molecule dimer disruptor

scientific article published on 26 July 2009

Inhibitors for the Vitamin D Receptor-Coregulator Interaction

scientific article published on 30 November 2015

Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships.

scientific article

Interaction between the androgen receptor and a segment of its corepressor SHP

scientific article

Ligand competition binding assay for the androgen receptor.

scientific article

MIDD0301 - A first-in-class anti-inflammatory asthma drug targets GABAA receptors without causing systemic immune suppression

scientific article published on 21 February 2019

Methylsulfonylnitrobenzoates, a new class of irreversible inhibitors of the interaction of the thyroid hormone receptor and its obligate coactivators that functionally antagonizes thyroid hormone.

scientific article

Modulation of Transcription mediated by the Vitamin D Receptor and the Peroxisome Proliferator-Activated Receptor δ in the presence of GW0742 analogs

scientific article published on January 2014

Novel Benzodiazepine-Like Ligands with Various Anxiolytic, Antidepressant, or Pro-Cognitive Profiles

scientific article published on 23 January 2019

Novel VDR antagonists based on the GW0742 scaffold

scientific article published on 19 December 2017

Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription

scientific article

Optimization of substituted imidazobenzodiazepines as novel asthma treatments

scientific article published on 24 November 2016

PT19c, Another Nonhypercalcemic Vitamin D2 Derivative, Demonstrates Antitumor Efficacy in Epithelial Ovarian and Endometrial Cancer Models.

scientific article

Parallel Chemistry Approach to Identify Novel Nuclear Receptor Ligands Based on the GW0742 Scaffold

scientific article published on 21 August 2017

Peroxisome proliferation-activated receptor δ agonist GW0742 interacts weakly with multiple nuclear receptors, including the vitamin D receptor

scientific article published on 10 June 2013

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

scientific article published on 4 March 2017

Quantification of the vitamin D receptor-coregulator interaction

scientific article

Similarities and differences between two modes of antagonism of the thyroid hormone receptor.

scientific article published on 15 August 2011

Structural insight into the mode of action of a direct inhibitor of coregulator binding to the thyroid hormone receptor

scientific article

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

Synthesis and biological evaluation of calcioic acid

scientific article published on 06 November 2019

Synthesis and characterization of BODIPY-labeled colchicine.

scientific article published on 20 July 2008

Synthesis and evaluation of vitamin D receptor-mediated activities of cholesterol and vitamin D metabolites

scientific article published on 6 January 2016

Synthesis of highly substituted dibenzo[b,f]azocines and their evaluation as protein kinase inhibitors

scientific article

Synthesis of medium ring heterocycles using an intramolecular Heck reaction

scientific article published on 01 August 2004

The Effects of pH on the Structure and Bioavailability of Imidazobenzodiazepine-3-Carboxylate MIDD0301

scientific article published on 26 February 2020

The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability

scientific article published on 29 June 2019

List of works by Leggy A Arnold

A Novel Orally Available Asthma Drug Candidate That Reduces Smooth Muscle Constriction and Inflammation by Targeting GABAA Receptors in the Lung.

A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model

A Structure-Activity Relationship Comparison of Imidazodiazepines Binding at Kappa, Mu, and Delta Opioid Receptors and the GABAA Receptor

A fluorescence-based high throughput assay for the determination of small molecule-human serum albumin protein binding

A high-throughput ligand competition binding assay for the androgen receptor and other nuclear receptors.

A high-throughput screening assay for pyruvate carboxylase.

A high-throughput screening method to identify small molecule inhibitors of thyroid hormone receptor coactivator binding

A new catalytic and enantioselective desymmetrization of symmetrical methylidene cycloalkene oxides

A novel GABAA receptor ligand MIDD0301 with limited blood-brain barrier penetration relaxes airway smooth muscle ex vivo and in vivo

A quantitative high-throughput screen identifies novel inhibitors of the interaction of thyroid receptor beta with a peptide of steroid receptor coactivator 2

A surface on the androgen receptor that allosterically regulates coactivator binding

Alleviation of Multiple Asthmatic Pathologic Features with Orally Available and Subtype Selective GABAA Receptor Modulators

Alternative binding sites at the vitamin D receptor and their ligands

An anthrone-based Kv7.2/7.3 channel blocker with improved properties for the investigation of psychiatric and neurodegenerative disorders

An integrated in vitro and in vivo high-throughput screen identifies treatment leads for ependymoma.

Anticancer activity of VDR-coregulator inhibitor PS121912.

Antitumor Activity of 3-Indolylmethanamines 31B and PS121912.

Calcitroic Acid-A Review.

Catalytic enantioselective synthesis of (-)-prostaglandin E1 methyl ester based on a tandem 1,4-addition-aldol reaction

Characterization of GABAA receptor ligands with automated patch-clamp using human neurons derived from pluripotent stem cells

Comparison of cell expression formats for the characterization of GABA(A) channels using a microfluidic patch clamp system

Copper phosphoramidite catalyzed enantioselective ring-opening of oxabicyclic alkenes: remarkable reversal of stereocontrol.

Correction to "A Novel Orally Available Asthma Drug Candidate That Reduces Smooth Muscle Constriction and Inflammation by Targeting GABAA Receptors in the Lung"

Design and Evaluation of Heterobivalent PAR1-PAR2 Ligands as Antagonists of Calcium Mobilization

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

Development of novel Vitamin D Receptor-Coactivator Inhibitors

Differential regulation of epidermal function by VDR coactivators

Discovery and Optimization of Novel Hydrogen Peroxide Activated Aromatic Nitrogen Mustard Derivatives as Highly Potent Anticancer Agents

Discovery of small molecule inhibitors of the interaction of the thyroid hormone receptor with transcriptional coregulators

Discovery of the first irreversible small molecule inhibitors of the interaction between the vitamin D receptor and coactivators

Efficacy of a non-hypercalcemic vitamin-D2 derived anti-cancer agent (MT19c) and inhibition of fatty acid synthesis in an ovarian cancer xenograft model

Enantioselective copper-catalyzed allylic alkylation with dialkylzincs using phosphoramidite ligands

Evaluation of the first Ergocalciferol-derived, non hypercalcemic anti-cancer agent MT19c in ovarian cancer SKOV-3 cell lines ⬇️

Further evaluation of the potential anxiolytic activity of imidazo[1,5-a][1,4]diazepin agents selective for α2/3-containing GABAA receptors

Genetic and pharmacological manipulation of glyoxalase 1 regulates voluntary ethanol consumption in mice

Glo1 inhibitors for neuropsychiatric and anti-epileptic drug development

High-throughput identification of promiscuous inhibitors from screening libraries with the use of a thiol-containing fluorescent probe

Highly Enantioselective Copper-Phosphoramidite Catalyzed Kinetic Resolution of Chiral 2-Cyclohexenones

Highly Enantioselective Copper-Phosphoramidite Catalyzed Kinetic Resolution of Chiral 2-Cyclohexenones This work was supported by the Dutch Foundation for Scientific Research (NWO)

Hydrogen peroxide activated quinone methide precursors with enhanced DNA cross-linking capability and cytotoxicity towards cancer cells.

IDENTIFICATION OF VDR ANTAGONISTS AMONG NUCLEAR RECEPTOR LIGANDS USING VIRTUAL SCREENING

Identification and analysis of hepatitis C virus NS3 helicase inhibitors using nucleic acid binding assays

Identification and characterization of the first small molecule inhibitor of MDMX

Identification of a Vitamin-D Receptor Antagonist, MeTC7, which Inhibits the Growth of Xenograft and Transgenic Tumors <i>In Vivo</i>

Identification of a novel, fast-acting GABAergic antidepressant

Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors.

Inhibition of a viral enzyme by a small-molecule dimer disruptor

Inhibitors for the Vitamin D Receptor-Coregulator Interaction

Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships.

Interaction between the androgen receptor and a segment of its corepressor SHP

Ligand competition binding assay for the androgen receptor.

MIDD0301 - A first-in-class anti-inflammatory asthma drug targets GABAA receptors without causing systemic immune suppression

Methylsulfonylnitrobenzoates, a new class of irreversible inhibitors of the interaction of the thyroid hormone receptor and its obligate coactivators that functionally antagonizes thyroid hormone.

Modulation of Transcription mediated by the Vitamin D Receptor and the Peroxisome Proliferator-Activated Receptor δ in the presence of GW0742 analogs

Novel Benzodiazepine-Like Ligands with Various Anxiolytic, Antidepressant, or Pro-Cognitive Profiles

Novel VDR antagonists based on the GW0742 scaffold

Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription

Optimization of substituted imidazobenzodiazepines as novel asthma treatments

PT19c, Another Nonhypercalcemic Vitamin D2 Derivative, Demonstrates Antitumor Efficacy in Epithelial Ovarian and Endometrial Cancer Models.

Parallel Chemistry Approach to Identify Novel Nuclear Receptor Ligands Based on the GW0742 Scaffold

Peroxisome proliferation-activated receptor δ agonist GW0742 interacts weakly with multiple nuclear receptors, including the vitamin D receptor

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

Quantification of the vitamin D receptor-coregulator interaction

Similarities and differences between two modes of antagonism of the thyroid hormone receptor.

Structural insight into the mode of action of a direct inhibitor of coregulator binding to the thyroid hormone receptor

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

Synthesis and biological evaluation of calcioic acid

Synthesis and characterization of BODIPY-labeled colchicine.

Synthesis and evaluation of vitamin D receptor-mediated activities of cholesterol and vitamin D metabolites

Synthesis of highly substituted dibenzo[b,f]azocines and their evaluation as protein kinase inhibitors

Synthesis of medium ring heterocycles using an intramolecular Heck reaction

The Effects of pH on the Structure and Bioavailability of Imidazobenzodiazepine-3-Carboxylate MIDD0301

The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability