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Applying Structure-Based Drug Design Approaches to Allosteric Modulators of GPCRs

Trends in pharmacological sciences (Regular ed.), 2017-09, Vol.38 (9), p.837-847

2017

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Generic GPCR residue numbers – aligning topology maps while minding the gaps

Trends in pharmacological sciences (Regular ed.), 2015-01, Vol.36 (1), p.22-31

2015

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From G Protein-coupled Receptor Structure Resolution to Rational Drug Design

The Journal of biological chemistry, 2015-08, Vol.290 (32), p.19489-19495

2015

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Structures of G protein-coupled receptors reveal new opportunities for drug discovery

Drug discovery today, 2015-11, Vol.20 (11), p.1355-1364

2015

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Structure of class B GPCR corticotropin-releasing factor receptor 1

Nature (London), 2013-07, Vol.499 (7459), p.438-443

2013

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Structure of the complement C5a receptor bound to the extra-helical antagonist NDT9513727

Nature (London), 2018-01, Vol.553 (7686), p.111-114

2018

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Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain

Nature (London), 2014-07, Vol.511 (7511), p.557-562

2014

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Crystal structure of the GLP-1 receptor bound to a peptide agonist

Nature (London), 2017-06, Vol.546 (7657), p.254-258

2017

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Extra-helical binding site of a glucagon receptor antagonist

Nature (London), 2016-05, Vol.533 (7602), p.274-277

2016

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Structurally Enabled Discovery of Adenosine A2A Receptor Antagonists

Chemical reviews, 2017-01, Vol.117 (1), p.21-37

2017

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Controlling the Dissociation of Ligands from the Adenosine A2A Receptor through Modulation of Salt Bridge Strength

Journal of medicinal chemistry, 2016-07, Vol.59 (13), p.6470-6479

2016

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Progress in Structure Based Drug Design for G Protein-Coupled Receptors

Journal of medicinal chemistry, 2011-07, Vol.54 (13), p.4283-4311

2011

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Towards high throughput GPCR crystallography: In Meso soaking of Adenosine A2A Receptor crystals

Scientific reports, 2018-01, Vol.8 (1), p.1-41, Article 41

2018

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Structure of Class B GPCRs: new horizons for drug discovery

British journal of pharmacology, 2014-07, Vol.171 (13), p.3132-3145

2014

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Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X‑ray Crystallography and Computational Analysis

Journal of medicinal chemistry, 2020-02, Vol.63 (4), p.1528-1543

2020

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Biophysical Fragment Screening of the β1‑Adrenergic Receptor: Identification of High Affinity Arylpiperazine Leads Using Structure-Based Drug Design

Journal of medicinal chemistry, 2013-05, Vol.56 (9), p.3446-3455

2013

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Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile)

Journal of medicinal chemistry, 2015-08, Vol.58 (16), p.6653-6664

2015

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Therapeutic antibodies directed at G protein-coupled receptors

mAbs, 2010-11, Vol.2 (6), p.594-606

2010

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Fragment Screening of Stabilized G-Protein-Coupled Receptors Using Biophysical Methods

Methods in Enzymology, 2011, Vol.493, p.115-136

2011

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Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors – A Structural Perspective of Ligands and Mutants

Scientific reports, 2015-09, Vol.5 (1), p.13869-13869, Article 13869

2015

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Conformational thermostabilisation of corticotropin releasing factor receptor 1

Scientific reports, 2015-07, Vol.5 (1), p.11954-11954, Article 11954

2015

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The Orphan G Protein-coupled Receptors GPR41 and GPR43 Are Activated by Propionate and Other Short Chain Carboxylic Acids

The Journal of biological chemistry, 2003-03, Vol.278 (13), p.11312-11319

2003

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Opportunities for therapeutic antibodies directed at G-protein-coupled receptors

Nature reviews. Drug discovery, 2017-11, Vol.16 (9), p.787-810

2017

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Safety, pharmacokinetics and exploratory pro-cognitive effects of HTL0018318, a selective M1 receptor agonist, in healthy younger adult and elderly subjects: a multiple ascending dose study

Alzheimer's research & therapy, 2021-04, Vol.13 (1), p.1-19, Article 87

2021

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Molecular Identification of High and Low Affinity Receptors for Nicotinic Acid

The Journal of biological chemistry, 2003-03, Vol.278 (11), p.9869-9874

2003

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Applying Structure-Based Drug Design Approaches to Allosteric Modulators of GPCRs

Generic GPCR residue numbers – aligning topology maps while minding the gaps

From G Protein-coupled Receptor Structure Resolution to Rational Drug Design

Structures of G protein-coupled receptors reveal new opportunities for drug discovery

Structure of class B GPCR corticotropin-releasing factor receptor 1

Structure of the complement C5a receptor bound to the extra-helical antagonist NDT9513727

Structure of class C GPCR metabotropic glutamate receptor 5 transmembrane domain

Crystal structure of the GLP-1 receptor bound to a peptide agonist

Extra-helical binding site of a glucagon receptor antagonist

Structurally Enabled Discovery of Adenosine A2A Receptor Antagonists

Controlling the Dissociation of Ligands from the Adenosine A2A Receptor through Modulation of Salt Bridge Strength

Progress in Structure Based Drug Design for G Protein-Coupled Receptors

Towards high throughput GPCR crystallography: In Meso soaking of Adenosine A2A Receptor crystals

Structure of Class B GPCRs: new horizons for drug discovery

Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X‑ray Crystallography and Computational Analysis

Biophysical Fragment Screening of the β1‑Adrenergic Receptor: Identification of High Affinity Arylpiperazine Leads Using Structure-Based Drug Design

Fragment and Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5 Negative Allosteric Modulator HTL14242 (3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile)

Therapeutic antibodies directed at G protein-coupled receptors

Fragment Screening of Stabilized G-Protein-Coupled Receptors Using Biophysical Methods

Selective Negative Allosteric Modulation Of Metabotropic Glutamate Receptors – A Structural Perspective of Ligands and Mutants

Conformational thermostabilisation of corticotropin releasing factor receptor 1

The Orphan G Protein-coupled Receptors GPR41 and GPR43 Are Activated by Propionate and Other Short Chain Carboxylic Acids

Opportunities for therapeutic antibodies directed at G-protein-coupled receptors

Safety, pharmacokinetics and exploratory pro-cognitive effects of HTL0018318, a selective M1 receptor agonist, in healthy younger adult and elderly subjects: a multiple ascending dose study

Molecular Identification of High and Low Affinity Receptors for Nicotinic Acid

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