List of works - David E. Gloriam

3-Substituted 2-phenyl-indoles: privileged structures for medicinal chemistry

article

5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology.

scientific article published on 19 January 2018

A Ligands View of Target Similarity: Chemogenomic Binding Site- Directed Techniques for Drug Discovery ⬇️

scientific article published on January 1, 2011

A Structural Framework for GPCR Chemogenomics: What's In a Residue Number?

scientific article published in January 2018

A community standard format for the representation of protein affinity reagents

scientific article

A new crystal structure fragment-based pharmacophore method for G protein-coupled receptors

scientific article

A novel red fluorescence dopamine biosensor selectively detects dopamine in the presence of norepinephrine in vitro

scientific article published on 06 December 2021

An online resource for GPCR structure determination and analysis

scientific article published on 21 January 2019

Applying label-free dynamic mass redistribution assay for studying endogenous FPR1 receptor signalling in human neutrophils

scientific article published on 14 July 2017

Author Correction: Combinatorial expression of GPCR isoforms affects signalling and drug responses

scientific article published on 25 November 2020

Bigger is better in virtual drug screens

scientific article published on 01 February 2019

Chemogenomic discovery of allosteric antagonists at the GPRC6A receptor

scientific article published on November 2011

Chemogenomics of allosteric binding sites in GPCRs

scientific article

Combinatorial expression of GPCR isoforms affects signalling and drug responses

scientific article published on 04 November 2020

Comprehensive comparisons of the current human, mouse, and rat RefSeq, Ensembl, EST, and FANTOM3 datasets: identification of new human genes with specific tissue expression profile

scientific article published on 4 August 2006

Comprehensive repertoire and phylogenetic analysis of the G protein-coupled receptors in human and mouse

scientific article

Computer-aided discovery of aromatic l-α-amino acids as agonists of the orphan G protein-coupled receptor GPR139.

scientific article published on 30 May 2014

Correction: Structure-Activity Relationships of Constrained Phenylethylamine Ligands for the Serotonin 5-HT2 Receptors.

scientific article published on 17 January 2014

Creating a specialist protein resource network: a meeting report for the protein bioinformatics and community resources retreat

scientific article

Critical evaluation of the FANTOM3 non-coding RNA transcripts

article

Definition of the G protein-coupled receptor transmembrane bundle binding pocket and calculation of receptor similarities for drug design.

scientific article

Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties

scientific article

Development of a human vasopressin V1a-receptor antagonist from an evolutionary-related insect neuropeptide.

scientific article published on February 2017

Discovery of 2-(Imidazo[1,2- b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites

scientific article published on 27 February 2019

Discovery of Human Signaling Systems: Pairing Peptides to G Protein-Coupled Receptors

scientific article published on 01 October 2019

Dynamic spatiotemporal determinants modulate GPCR:G protein coupling selectivity and promiscuity

scientific article published in 2022

Editorial [Hot Topic: Methods for the Successful Application of Chemogenomics to GPCR Drug Design (Guest Editors: Stephen L. Garland & David E. Gloriam)]

scientific article published on 01 January 2011

Editorial overview: New technologies: GPCR drug design and function — exploiting the current (of) structures

scholarly article by Christofer S. Tautermann & David E. Gloriam published October 2016 in Current Opinion in Pharmacology

Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters

scientific article published on 05 June 2019

G protein- and agonist-bound serotonin 5-HT2A receptor model activated by steered molecular dynamics simulations

scientific article

GPCRDB: an information system for G protein-coupled receptors

scientific article (published in December 2013)

GPCRdb in 2018: adding GPCR structure models and ligands.

scientific article published on 16 November 2017

GPCRdb: an information system for G protein-coupled receptors.

scientific article published on 17 November 2015

GPCRmd uncovers the dynamics of the 3D-GPCRome

scientific article published on 13 July 2020

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

scientific article

High species variation within the repertoire of trace amine receptors.

scientific article

Identification and characterization of small molecular NPR-B receptor antagonists.

scientific article published on 2 September 2015

Identification of Histamine H3 Receptor Ligands Using a New Crystal Structure Fragment-based Method.

scientific article published on 6 July 2017

Identification of a novel scaffold for a small molecule GPR139 receptor agonist

scientific article published on 07 March 2019

Identification of the first surrogate agonists for the G protein-coupled receptor GPR132

article

In Silico Identification of Novel G Protein-Coupled Receptors

Integrating structural and mutagenesis data to elucidate GPCR ligand binding.

scientific article

Minimum information about a protein affinity reagent (MIAPAR)

scientific article published on 01 July 2010

Modulation in Selectivity and Allosteric Properties of Small-Molecule Ligands for CC-Chemokine Receptors

Molecular Hybridization of Potent and Selective γ-Hydroxybutyric Acid (GHB) Ligands: Design, Synthesis, Binding Studies, and Molecular Modeling of Novel 3-Hydroxycyclopent-1-enecarboxylic Acid (HOCPCA) and trans-γ-Hydroxycrotonic Acid (T-HCA) Analog

scientific article

Nine new human Rhodopsin family G-protein coupled receptors: identification, sequence characterisation and evolutionary relationship

scientific article

Novel Agonist Bioisosteres and Common Structure-Activity Relationships for The Orphan G Protein-Coupled Receptor GPR139.

scientific article published on 10 November 2016

Novel approaches leading towards peptide GPCR de-orphanisation

scientific article published on 03 February 2020

Pharmacogenomics of GPCR Drug Targets

scientific article published on 8 December 2017

Pharmacological characterization and modeling of the binding sites of novel 1,3-bis(pyridinylethynyl)benzenes as metabotropic glutamate receptor 5-selective negative allosteric modulators

scientific article published on 16 August 2012

Present perspectives on the automated classification of the G-protein coupled receptors (GPCRs) at the protein sequence level

scientific article published on January 2011

Probing the Existence of a Metastable Binding Site at the β2-Adrenergic Receptor with Homobivalent Bitopic Ligands

scientific article published on 15 August 2019

ProteomeBinders: planning a European resource of affinity reagents for analysis of the human proteome

article

Proteomic applications of automated GPCR classification

scientific article published on August 2007

Publisher Correction: GPCRmd uncovers the dynamics of the 3D-GPCRome

scientific article published on 23 July 2020

Rational design of a heterotrimeric G protein α subunit with artificial inhibitor sensitivity

scientific article published on 11 February 2019

Receptor selectivity between the G proteins Gα and Gα is defined by a single leucine-to-isoleucine variation

scientific article published on 02 January 2019

SMARTCyp: A 2D Method for Prediction of Cytochrome P450-Mediated Drug Metabolism

scientific article (publication date: 10 June 2010)

Selective Allosteric Antagonists for the G Protein-Coupled Receptor GPRC6A Based on the 2-Phenylindole Privileged Structure Scaffold

scientific article published on 30 October 2015

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

scientific article published on 11 September 2015

Selectivity determinants of GPCR-G-protein binding

scientific article published on 10 May 2017

Seven evolutionarily conserved human rhodopsin G protein-coupled receptors lacking close relatives

scientific article (publication date: 20 November 2003)

Structural Mapping of Adenosine Receptor Mutations: Ligand Binding and Signaling Mechanisms

scientific article published in December 2017

Structural insight to mutation effects uncover a common allosteric site in class C GPCRs

scientific article published on 22 December 2016

Structural insights into the lipid and ligand regulation of serotonin receptors

Structure of the class D GPCR Ste2 dimer coupled to two G proteins

scientific article published on 02 December 2020

Structure-activity relationships and identification of optmized CC-chemokine receptor CCR1, 5, and 8 metal-ion chelators

scientific article published on 22 October 2013

Structure-activity relationships for negative allosteric mGluR5 modulators

scientific article

Structure-activity relationships of constrained phenylethylamine ligands for the serotonin 5-HT2 receptors

scientific article (publication date: 2013)

Structure–activity relationship and conformational studies of the natural product cyclic depsipeptides YM-254890 and FR900359

scientific article published on 12 July 2018

Targeting the APP-Mint2 Protein-Protein Interaction with a Peptide-Based Inhibitor Reduces Amyloid-β Formation

scientific article published on 05 January 2021

The G protein-coupled receptor subset of the chicken genome

scientific article published in June 2006

The G protein-coupled receptor subset of the dog genome is more similar to that in humans than rodents

scientific article

The G protein-coupled receptor subset of the rat genome

scientific article

The GPR139 reference agonists 1a and 7c, and tryptophan and phenylalanine share a common binding site

scientific article

The SMARTCyp cytochrome P450 metabolism prediction server

scientific article

The contribution of atom accessibility to site of metabolism models for cytochromes P450.

scientific article published on 22 January 2013

The human and mouse repertoire of the adhesion family of G-protein-coupled receptors

scientific article

The orphan G protein-coupled receptor GPR139 is activated by the peptides: Adrenocorticotropic hormone (ACTH), α-, and β-melanocyte stimulating hormone (α-MSH, and β-MSH), and the conserved core motif HFRW.

scientific article published on December 2016

The repertoire of trace amine G-protein-coupled receptors: large expansion in zebrafish

scientific article

There exist at least 30 human G-protein-coupled receptors with long Ser/Thr-rich N-termini

scientific article

Total synthesis and structure-activity relationship studies of a series of selective G protein inhibitors

scientific article published on 25 July 2016

Trends in GPCR drug discovery: new agents, targets and indications.

scientific article

mGluR5: exploration of orthosteric and allosteric ligand binding pockets and their applications to drug discovery

scientific article

List of works by David E. Gloriam

3-Substituted 2-phenyl-indoles: privileged structures for medicinal chemistry

5-HT2C Receptor Structures Reveal the Structural Basis of GPCR Polypharmacology.

A Ligands View of Target Similarity: Chemogenomic Binding Site- Directed Techniques for Drug Discovery ⬇️

A Structural Framework for GPCR Chemogenomics: What's In a Residue Number?

A community standard format for the representation of protein affinity reagents

A new crystal structure fragment-based pharmacophore method for G protein-coupled receptors

A novel red fluorescence dopamine biosensor selectively detects dopamine in the presence of norepinephrine in vitro

An online resource for GPCR structure determination and analysis

Applying label-free dynamic mass redistribution assay for studying endogenous FPR1 receptor signalling in human neutrophils

Author Correction: Combinatorial expression of GPCR isoforms affects signalling and drug responses

Bigger is better in virtual drug screens

Chemogenomic discovery of allosteric antagonists at the GPRC6A receptor

Chemogenomics of allosteric binding sites in GPCRs

Combinatorial expression of GPCR isoforms affects signalling and drug responses

Comprehensive comparisons of the current human, mouse, and rat RefSeq, Ensembl, EST, and FANTOM3 datasets: identification of new human genes with specific tissue expression profile

Comprehensive repertoire and phylogenetic analysis of the G protein-coupled receptors in human and mouse

Computer-aided discovery of aromatic l-α-amino acids as agonists of the orphan G protein-coupled receptor GPR139.

Correction: Structure-Activity Relationships of Constrained Phenylethylamine Ligands for the Serotonin 5-HT2 Receptors.

Creating a specialist protein resource network: a meeting report for the protein bioinformatics and community resources retreat

Critical evaluation of the FANTOM3 non-coding RNA transcripts

Definition of the G protein-coupled receptor transmembrane bundle binding pocket and calculation of receptor similarities for drug design.

Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol analogues: novel 5-HT(2A)/5-HT(2C) receptor agonists with pro-cognitive properties

Development of a human vasopressin V1a-receptor antagonist from an evolutionary-related insect neuropeptide.

Discovery of 2-(Imidazo[1,2- b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites

Discovery of Human Signaling Systems: Pairing Peptides to G Protein-Coupled Receptors

Dynamic spatiotemporal determinants modulate GPCR:G protein coupling selectivity and promiscuity

Editorial [Hot Topic: Methods for the Successful Application of Chemogenomics to GPCR Drug Design (Guest Editors: Stephen L. Garland & David E. Gloriam)]

Editorial overview: New technologies: GPCR drug design and function — exploiting the current (of) structures

Five-Membered N-Heterocyclic Scaffolds as Novel Amino Bioisosteres at γ-Aminobutyric Acid (GABA) Type A Receptors and GABA Transporters

G protein- and agonist-bound serotonin 5-HT2A receptor model activated by steered molecular dynamics simulations

GPCRDB: an information system for G protein-coupled receptors

GPCRdb in 2018: adding GPCR structure models and ligands.

GPCRdb: an information system for G protein-coupled receptors.

GPCRmd uncovers the dynamics of the 3D-GPCRome

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

High species variation within the repertoire of trace amine receptors.

Identification and characterization of small molecular NPR-B receptor antagonists.

Identification of Histamine H3 Receptor Ligands Using a New Crystal Structure Fragment-based Method.

Identification of a novel scaffold for a small molecule GPR139 receptor agonist

Identification of the first surrogate agonists for the G protein-coupled receptor GPR132

In Silico Identification of Novel G Protein-Coupled Receptors

Integrating structural and mutagenesis data to elucidate GPCR ligand binding.

Minimum information about a protein affinity reagent (MIAPAR)

Modulation in Selectivity and Allosteric Properties of Small-Molecule Ligands for CC-Chemokine Receptors

Molecular Hybridization of Potent and Selective γ-Hydroxybutyric Acid (GHB) Ligands: Design, Synthesis, Binding Studies, and Molecular Modeling of Novel 3-Hydroxycyclopent-1-enecarboxylic Acid (HOCPCA) and trans-γ-Hydroxycrotonic Acid (T-HCA) Analog

Nine new human Rhodopsin family G-protein coupled receptors: identification, sequence characterisation and evolutionary relationship

Novel Agonist Bioisosteres and Common Structure-Activity Relationships for The Orphan G Protein-Coupled Receptor GPR139.

Novel approaches leading towards peptide GPCR de-orphanisation

Pharmacogenomics of GPCR Drug Targets

Pharmacological characterization and modeling of the binding sites of novel 1,3-bis(pyridinylethynyl)benzenes as metabotropic glutamate receptor 5-selective negative allosteric modulators

Present perspectives on the automated classification of the G-protein coupled receptors (GPCRs) at the protein sequence level

Probing the Existence of a Metastable Binding Site at the β2-Adrenergic Receptor with Homobivalent Bitopic Ligands

ProteomeBinders: planning a European resource of affinity reagents for analysis of the human proteome

Proteomic applications of automated GPCR classification

Publisher Correction: GPCRmd uncovers the dynamics of the 3D-GPCRome

Rational design of a heterotrimeric G protein α subunit with artificial inhibitor sensitivity

Receptor selectivity between the G proteins Gα and Gα is defined by a single leucine-to-isoleucine variation

SMARTCyp: A 2D Method for Prediction of Cytochrome P450-Mediated Drug Metabolism

Selective Allosteric Antagonists for the G Protein-Coupled Receptor GPRC6A Based on the 2-Phenylindole Privileged Structure Scaffold

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

Selectivity determinants of GPCR-G-protein binding

Seven evolutionarily conserved human rhodopsin G protein-coupled receptors lacking close relatives

Structural Mapping of Adenosine Receptor Mutations: Ligand Binding and Signaling Mechanisms

Structural insight to mutation effects uncover a common allosteric site in class C GPCRs

Structural insights into the lipid and ligand regulation of serotonin receptors

Structure of the class D GPCR Ste2 dimer coupled to two G proteins

Structure-activity relationships and identification of optmized CC-chemokine receptor CCR1, 5, and 8 metal-ion chelators

Structure-activity relationships for negative allosteric mGluR5 modulators

Structure-activity relationships of constrained phenylethylamine ligands for the serotonin 5-HT2 receptors

Structure–activity relationship and conformational studies of the natural product cyclic depsipeptides YM-254890 and FR900359

Targeting the APP-Mint2 Protein-Protein Interaction with a Peptide-Based Inhibitor Reduces Amyloid-β Formation

The G protein-coupled receptor subset of the chicken genome

The G protein-coupled receptor subset of the dog genome is more similar to that in humans than rodents

The G protein-coupled receptor subset of the rat genome

The GPR139 reference agonists 1a and 7c, and tryptophan and phenylalanine share a common binding site

The SMARTCyp cytochrome P450 metabolism prediction server

The contribution of atom accessibility to site of metabolism models for cytochromes P450.

The human and mouse repertoire of the adhesion family of G-protein-coupled receptors

The orphan G protein-coupled receptor GPR139 is activated by the peptides: Adrenocorticotropic hormone (ACTH), α-, and β-melanocyte stimulating hormone (α-MSH, and β-MSH), and the conserved core motif HFRW.