List of works - Steven J. Charlton

'Partial' competition of heterobivalent ligand binding may be mistaken for allosteric interactions: a comparison of different target interaction models.

scientific article published on 17 March 2015

A single point mutation (N514Y) in the human M3 muscarinic acetylcholine receptor reveals differences in the properties of antagonists: evidence for differential inverse agonism.

scientific article published on 17 February 2006

Agonist efficacy and receptor desensitization: from partial truths to a fuller picture.

scientific article published on September 2009

Agonist-biased signaling at the histamine H4 receptor: JNJ7777120 recruits β-arrestin without activating G proteins.

scientific article published on 6 December 2010

Airway remodeling disease: primary human structural cells and phenotypic and pathway assays to identify targets with potential to prevent or reverse remodeling

An Alternative Thiol-Reactive Dye to Analyze Ligand Interactions with the Chemokine Receptor CXCR2 Using a New Thermal Shift Assay Format

scientific article published on 7 December 2015

An investigation into the structure-activity relationships associated with the systematic modification of the β(2)-adrenoceptor agonist indacaterol.

scientific article

Analysis of multiple histamine H₄ receptor compound classes uncovers Gαi protein- and β-arrestin2-biased ligands

scientific article published on 12 September 2012

Analysis of second messenger pathways stimulated by different chemokines acting at the chemokine receptor CCR5.

scientific article published on 20 June 2007

BJP issue on drug discovery.

scientific article published on November 2010

Comparing the cardiovascular therapeutic indices of glycopyrronium and tiotropium in an integrated rat pharmacokinetic, pharmacodynamic and safety model

scientific article published on 27 May 2015

Design and synthesis of a library of chemokine antagonists ⬇️

scientific article published on September 10, 2011

Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma

scientific article published on 25 April 2017

Efficacy is a contributing factor to the clinical onset of bronchodilation of inhaled beta(2)-adrenoceptor agonists.

scientific article published on 8 August 2010

Elusive equilibrium: the challenge of interpreting receptor pharmacology using calcium assays.

scientific article

Endomorphin-2: a biased agonist at the μ-opioid receptor.

scientific article

Enhancement of the response to purinergic agonists in P2Y1 transfected 1321N1 cells by antagonists suramin and PPADS.

scientific article published on March 1997

Evidence that P2Y4 nucleotide receptors are involved in the regulation of rat aortic smooth muscle cells by UTP and ATP.

scientific article published in June 1998

Exploring avidity: understanding the potential gains in functional affinity and target residence time of bivalent and heterobivalent ligands ⬇️

scientific article published on April 1, 2013

Exploring the mechanism of agonist efficacy: a relationship between efficacy and agonist dissociation rate at the muscarinic M3 receptor.

scientific article published on 4 June 2009

Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors

scientific article published on 2 October 2017

Fevipiprant (QAW039), a Slowly Dissociating CRTh2 Antagonist with the Potential for Improved Clinical Efficacy.

scientific article

HDL-like discs for assaying membrane proteins in drug discovery

scientific article published on 19 March 2012

High throughput mutagenesis for identification of residues regulating human prostacyclin (hIP) receptor expression and function

scientific article (publication date: 2014)

Identification of novel IP receptor agonists using historical ligand biased chemical arrays

scientific article published on 05 April 2014

In vitro and in vivo pharmacological characterization of 5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one (indacaterol), a novel inhaled beta(2) adrenoceptor agonist with a 24-h duration of action

scientific article published on 24 January 2006

Investigating the molecular mechanisms through which FTY720-P causes persistent S1P1 receptor internalization

scientific article published on November 2014

Long Receptor Residence Time of C26 Contributes to Super Agonist Activity at the Human β2 Adrenoceptor.

scientific article published on 15 January 2016

Long‐lasting target binding and rebinding as mechanisms to prolong in vivo drug action ⬇️

scientific article published on October 1, 2010

Measuring receptor target coverage: a radioligand competition binding protocol for assessing the association and dissociation rates of unlabeled compounds

scientific article published in September 2010

Micro-pharmacokinetics: Quantifying local drug concentration at live cell membranes

scientific article published on 22 February 2018

Miniaturized receptor binding assays: complications arising from ligand depletion

scientific article published on 26 January 2007

Observed drug-receptor association rates are governed by membrane affinity: the importance of establishing "micro-pharmacokinetic/pharmacodynamic relationships" at the β2-adrenoceptor

scientific article published on 29 January 2014

PPARgamma is not a critical mediator of primary monocyte differentiation or foam cell formation.

scientific article

Potent and efficacious inhibition of CXCR2 signaling by biparatopic nanobodies combining two distinct modes of action.

scientific article published on 2 December 2014

Quantifying the association and dissociation rates of unlabelled antagonists at the muscarinic M3 receptor.

scientific article published on 10 July 2006

Reassessment of the pharmacology of Sphingosine-1-phosphate S1P3 receptor ligands using the DiscoveRx PathHunter™ and Ca2+ release functional assays.

scientific article published on October 2012

Reply to 'Antipsychotics with similar association kinetics at dopamine D receptors differ in extrapyramidal side-effects'

scientific article published in Nature Communications

Simulating the influence of plasma protein on measured receptor affinity in biochemical assays reveals the utility of Schild analysis for estimating compound affinity for plasma proteins.

scientific article published on 24 July 2015

Slow receptor dissociation is not a key factor in the duration of action of inhaled long-acting β2-adrenoceptor agonists

scientific article published on April 2012

Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists

scientific article published in December 2009

The Influence of receptor kinetics on the onset and duration of action and the therapeutic index of NVA237 and tiotropium

scientific article published in August 2012

The antiallergic mast cell stabilizers lodoxamide and bufrolin as the first high and equipotent agonists of human and rat GPR35

scientific article published on 10 October 2013

The discovery of potent, orally bioavailable pyrazolo and triazolopyrimidine CXCR2 receptor antagonists.

scientific article

The discovery of potent, orally bioavailable pyrimidine-5-carbonitrile-6-alkyl CXCR2 receptor antagonists.

scientific article

The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist

scientific article

The in vitro metabolism of sphingosine-1-phosphate: identification; inhibition and pharmacological implications.

scientific article published on 29 September 2011

The long-acting beta-adrenoceptor agonist, indacaterol, inhibits IgE-dependent responses of human lung mast cells

scientific article published on 09 April 2009

The role of kinetic context in apparent biased agonism at GPCRs

scientific article published on 24 February 2016

Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.

scientific article published on 30 May 2016

μ-opioid receptors: correlation of agonist efficacy for signalling with ability to activate internalization

scientific article

List of works by Steven J. Charlton

'Partial' competition of heterobivalent ligand binding may be mistaken for allosteric interactions: a comparison of different target interaction models.

A single point mutation (N514Y) in the human M3 muscarinic acetylcholine receptor reveals differences in the properties of antagonists: evidence for differential inverse agonism.

Agonist efficacy and receptor desensitization: from partial truths to a fuller picture.

Agonist-biased signaling at the histamine H4 receptor: JNJ7777120 recruits β-arrestin without activating G proteins.

Airway remodeling disease: primary human structural cells and phenotypic and pathway assays to identify targets with potential to prevent or reverse remodeling

An Alternative Thiol-Reactive Dye to Analyze Ligand Interactions with the Chemokine Receptor CXCR2 Using a New Thermal Shift Assay Format

An investigation into the structure-activity relationships associated with the systematic modification of the β(2)-adrenoceptor agonist indacaterol.

Analysis of multiple histamine H₄ receptor compound classes uncovers Gαi protein- and β-arrestin2-biased ligands

Analysis of second messenger pathways stimulated by different chemokines acting at the chemokine receptor CCR5.

BJP issue on drug discovery.

Comparing the cardiovascular therapeutic indices of glycopyrronium and tiotropium in an integrated rat pharmacokinetic, pharmacodynamic and safety model

Design and synthesis of a library of chemokine antagonists ⬇️

Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma

Efficacy is a contributing factor to the clinical onset of bronchodilation of inhaled beta(2)-adrenoceptor agonists.

Elusive equilibrium: the challenge of interpreting receptor pharmacology using calcium assays.

Endomorphin-2: a biased agonist at the μ-opioid receptor.

Enhancement of the response to purinergic agonists in P2Y1 transfected 1321N1 cells by antagonists suramin and PPADS.

Evidence that P2Y4 nucleotide receptors are involved in the regulation of rat aortic smooth muscle cells by UTP and ATP.

Exploring avidity: understanding the potential gains in functional affinity and target residence time of bivalent and heterobivalent ligands ⬇️

Exploring the mechanism of agonist efficacy: a relationship between efficacy and agonist dissociation rate at the muscarinic M3 receptor.

Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors

Fevipiprant (QAW039), a Slowly Dissociating CRTh2 Antagonist with the Potential for Improved Clinical Efficacy.

HDL-like discs for assaying membrane proteins in drug discovery

High throughput mutagenesis for identification of residues regulating human prostacyclin (hIP) receptor expression and function

Identification of novel IP receptor agonists using historical ligand biased chemical arrays

In vitro and in vivo pharmacological characterization of 5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-one (indacaterol), a novel inhaled beta(2) adrenoceptor agonist with a 24-h duration of action

Investigating the molecular mechanisms through which FTY720-P causes persistent S1P1 receptor internalization

Long Receptor Residence Time of C26 Contributes to Super Agonist Activity at the Human β2 Adrenoceptor.

Long‐lasting target binding and rebinding as mechanisms to prolong in vivo drug action ⬇️

Measuring receptor target coverage: a radioligand competition binding protocol for assessing the association and dissociation rates of unlabeled compounds

Micro-pharmacokinetics: Quantifying local drug concentration at live cell membranes

Miniaturized receptor binding assays: complications arising from ligand depletion

Observed drug-receptor association rates are governed by membrane affinity: the importance of establishing "micro-pharmacokinetic/pharmacodynamic relationships" at the β2-adrenoceptor

PPARgamma is not a critical mediator of primary monocyte differentiation or foam cell formation.

Potent and efficacious inhibition of CXCR2 signaling by biparatopic nanobodies combining two distinct modes of action.

Quantifying the association and dissociation rates of unlabelled antagonists at the muscarinic M3 receptor.

Reassessment of the pharmacology of Sphingosine-1-phosphate S1P3 receptor ligands using the DiscoveRx PathHunter™ and Ca2+ release functional assays.

Reply to 'Antipsychotics with similar association kinetics at dopamine D receptors differ in extrapyramidal side-effects'

Simulating the influence of plasma protein on measured receptor affinity in biochemical assays reveals the utility of Schild analysis for estimating compound affinity for plasma proteins.

Slow receptor dissociation is not a key factor in the duration of action of inhaled long-acting β2-adrenoceptor agonists

Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists

The Influence of receptor kinetics on the onset and duration of action and the therapeutic index of NVA237 and tiotropium

The antiallergic mast cell stabilizers lodoxamide and bufrolin as the first high and equipotent agonists of human and rat GPR35

The discovery of potent, orally bioavailable pyrazolo and triazolopyrimidine CXCR2 receptor antagonists.

The discovery of potent, orally bioavailable pyrimidine-5-carbonitrile-6-alkyl CXCR2 receptor antagonists.

The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist

The in vitro metabolism of sphingosine-1-phosphate: identification; inhibition and pharmacological implications.

The long-acting beta-adrenoceptor agonist, indacaterol, inhibits IgE-dependent responses of human lung mast cells

The role of kinetic context in apparent biased agonism at GPCRs

Uncoupling the Structure-Activity Relationships of β2 Adrenergic Receptor Ligands from Membrane Binding.

μ-opioid receptors: correlation of agonist efficacy for signalling with ability to activate internalization