S. Charlton

发表

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

M. Dowling, S. Charlton, 2006, British journal of pharmacology.

Exploring the Mechanism of Agonist Efficacy: A Relationship between Efficacy and Agonist Dissociation Rate at the Muscarinic M3 Receptor

M. Dowling, S. Charlton, D. Sykes, 2009, Molecular Pharmacology.

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

S. Charlton, G. Vauquelin, Georges Vauquelin, 2013, British journal of pharmacology.

Expression and characterization of a 5-oxo-6E,8Z,11Z,14Z-eicosatetraenoic acid receptor highly expressed on human eosinophils and neutrophils.

N. Nirmala, K. Seuwen, S. Charlton, 2003, Molecular pharmacology.

Exploring the kinetic selectivity of drugs targeting the β1‐adrenoceptor

D. Veprintsev, S. Charlton, D. Sykes, 2021, bioRxiv.

A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators.

B. Cuenoud, R. Taylor, S. Charlton, 2010, Bioorganic & medicinal chemistry letters.

The Preclinical Pharmacology of Indacaterol

S. Charlton, A. Trifilieff, R. A. Fairhurst, 2014 .

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

S. Charlton, 2009, British journal of pharmacology.

Investigating the molecular mechanisms through which FTY 720P causes persistent S 1 P 1 receptor internalisation 1

M. Dowling, S. Charlton, A. Sattikar, 2014 .

Pharmacological Characterization of a Novel 5-Hydroxybenzothiazolone-Derived β2-Adrenoceptor Agonist with Functional Selectivity for Anabolic Effects on Skeletal Muscle Resulting in a Wider Cardiovascular Safety Window in Preclinical Studies

S. Hatakeyama, T. Ullrich, D. Glass, 2019, The Journal of Pharmacology and Experimental Therapeutics.

Reply to ‘Antipsychotics with similar association kinetics at dopamine D2 receptors differ in extrapyramidal side-effects’

J. R. Lane, J. Javitch, S. Charlton, 2018, Nature Communications.

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

S. Briddon, S. Charlton, K. Gherbi, 2018, Scientific Reports.

The characterisation of cloned P2Y receptors transfected into 1321N1 astrocytoma cells

S. Charlton, 1998 .

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

Callum J. Dickson, V. Hornak, S. Charlton, 2016, Journal of medicinal chemistry.

Biased Agonism in Drug Discovery—Is It Too Soon to Choose a Path?

S. Charlton, M. Michel, 2018, Molecular Pharmacology.

The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist.

J. Fozard, B. Faller, D. Wyss, 2010, Journal of medicinal chemistry.

Efficacy is a contributing factor to the clinical onset of bronchodilation of inhaled β2-adrenoceptor agonists

S. Charlton, R. A. Fairhurst, E. Rosethorne, 2010, Naunyn-Schmiedeberg's Archives of Pharmacology.

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

S. Charlton, A. Sattikar, D. Sykes, 2016, Molecular Pharmacology.

Potent and Efficacious Inhibition of CXCR2 Signaling by Biparatopic Nanobodies Combining Two Distinct Modes of Action

S. Charlton, T. Laeremans, B. Dombrecht, 2015, Molecular Pharmacology.

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

S. Charlton, G. Vauquelin, David Hall, 2015, British journal of pharmacology.

PPARγ Is Not a Critical Mediator of Primary Monocyte Differentiation or Foam Cell Formation

S. J. Newman, J. Clapham, Stephen A. Smith, 2002 .

Investigating the Influence of Tracer Kinetics on Competition-Kinetic Association Binding Assays: Identifying the Optimal Conditions for Assessing the Kinetics of Low-Affinity Compounds

S. Charlton, D. Sykes, Palash Jain, 2019, Molecular Pharmacology.

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

S. Charlton, D. Sykes, 2012, British journal of pharmacology.

THEMED ISSUE: GPCR RESEARCH PAPER Pharmacogenetic characterization of indacaterol, a novel b2-adrenoceptor agonist

I. Sayers, A. Henry, S. Charlton, 2009 .

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

S. Watson, S. Charlton, D. Sykes, 2016, Molecular Pharmacology.

Fevipiprant ( QAW 039 ) , a Slowly Dissociating CRTh 2 Antagonist with the Potential for Improved Clinical Efficacy s

S. Watson, S. Charlton, D. Sykes, 2016 .

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

D. Budd, S. Watson, S. Charlton, 2017, ACS medicinal chemistry letters.

Detailed analysis of biased histamine H4 receptor signalling by JNJ 7777120 analogues

R. Leurs, S. Charlton, S. Schultes, 2013, British journal of pharmacology.

Functional desensitization of the b 2 adrenoceptor is not dependent on agonist efﬁcacy

S. Charlton, M. Bradley, E. Rosethorne, 2015 .

HDL-like discs for assaying membrane proteins in drug discovery.

U. Schopfer, S. Charlton, D. Sykes, 2012, Biophysical chemistry.

In Vitro and in Vivo Pharmacological Characterization of 5-[ ( R )-2-( 5 , 6-Diethyl-indan-2-ylamino )-1-hydroxyethyl ]-8-hydroxy-1 H-quinolin-2one ( Indacaterol ) , a Novel Inhaled 2 Adrenoceptor Agonist with a 24h Duration of Action

J. Fozard, C. Battram, B. Cuenoud, 2006 .

The Design of the Indacaterol Molecule

S. Charlton, A. Trifilieff, R. A. Fairhurst, 2014 .

The inhibition of human lung fibroblast proliferation and differentiation by Gs-coupled receptors is not predicted by the magnitude of cAMP response

R. Broome, S. Charlton, Maxine J. Roberts, 2018, Respiratory Research.

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

S. Charlton, L. Ng, M. Boarder, 1998, British journal of pharmacology.

F1000Prime recommendation of Formation and dissociation of M1 muscarinic receptor dimers seen by total internal reflection fluorescence imaging of single molecules.

S. Charlton, M. Bradley, 2010 .

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

S. Charlton, P. Strange, K. Leach, 2007, Biochemical pharmacology.

PPADS and suramin as antagonists at cloned P2Y‐ and P2U‐purinoceptors

J. T. Turner, S. Charlton, G. Weisman, 1996, British journal of pharmacology.

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

M. Dowling, S. Charlton, D. Sykes, 2012, British journal of pharmacology.

Running Title : Super Agonism at the β 2 Adrenoceptor

S. Charlton, A. Trifilieff, R. A. Fairhurst, 2017 .

Title : Long Receptor Residence Time of C 26 Contributes to Super Agonist Activity at the Human β 2 Adrenoceptor

S. Charlton, A. Sattikar, D. Sykes, 2016 .

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

M. Dowling, S. Charlton, M. Bradley, 2011, European journal of pharmacology.

A Single Point Mutation (N514Y) in the Human M3 Muscarinic Acetylcholine Receptor Reveals Differences in the Properties of Antagonists: Evidence for Differential Inverse Agonism

R. Challiss, D. Budd, M. Dowling, 2006, Journal of Pharmacology and Experimental Therapeutics.

Microsoft Word-40549129-file00

M. Dowling, S. Charlton, D. Sykes, 2009 .

The role of kinetic context in apparent biased agonism at GPCRs

Arthur Christopoulos, Patrick M Sexton, Jonathan A Javitch, 2016, Nature Communications.

Chemokines and drug discovery.

S. Charlton, S. Hodgson, Peter Warne, 2004, Drug news & perspectives.

Endomorphin-2: A Biased Agonist at the μ-Opioid Receptor

S. Mundell, C. McArdle, S. Charlton, 2012, Molecular Pharmacology.

Agonist-biased signalling at the histamine H 4 receptor : JNJ 7777120 recruits beta-arrestin without activating G proteins

S. Charlton, E. Rosethorne, 2010 .

Analysis of Multiple Histamine H 4 Receptor Compound Classes Uncovers G (cid:1) i Protein- and (cid:2) -Arrestin2-Biased Ligands □ S

R. Leurs, H. Vischer, S. Charlton, 2012 .

Mass spectrometry captures biased signalling and allosteric modulation of a G-protein-coupled receptor

C. Robinson, M. Sansom, P. Kapoor, 2022, Nature chemistry.

Cloned and transfected P2Y4 receptors: characterization of a suramin and PPADS‐insensitive response to UTP

J. T. Turner, S. Charlton, G. Weisman, 1996, British journal of pharmacology.

μ-Opioid Receptors: Correlation of Agonist Efficacy for Signalling with Ability to Activate Internalization

S. Charlton, C. Krasel, W. Dewey, 2010, Molecular Pharmacology.

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

C. Leblanc, S. Charlton, Arndt Meyer, 2014, Bioorganic & medicinal chemistry letters.

Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor.

Shailesh N Mistry, S. Charlton, D. Sykes, 2019, Journal of medicinal chemistry.

Assessing the minimum number of data points required for accurate IC50 determination.

S. Charlton, Steven J Charlton, Robert J Turner, 2005, Assay and drug development technologies.

The M3-muscarinic receptor regulates learning and memory in a receptor phosphorylation/arrestin-dependent manner

J. Wess, A. Tobin, B. Poulin, 2010, Proceedings of the National Academy of Sciences.

Interaction With the Lipid Membrane Influences Fentanyl Pharmacology

R. Sessions, S. Charlton, R. Corey, 2022, Advances in Drug and Alcohol Research.

Responses of the longitudinal muscle and the muscularis mucosae of the rat duodenum to adenine and uracil nucleotides

S. Charlton, S. Hourani, C. Johnson, 1996, British journal of pharmacology.

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

J. Fozard, S. Charlton, P. Gedeck, 2010, Bioorganic & medicinal chemistry letters.

Expression and functional analysis of chemokine receptors in human peripheral blood leukocyte populations.

J. Chambers, S. Charlton, C. Macphee, 2001, Cytokine.

Using NanoBit complementation and TR FRET to Study the Mechanism of Action of Small‐molecule Modulators of CXCR2

D. Nesheva, N. Holliday, S. Charlton, 2020, The FASEB Journal.

Miniaturized Receptor Binding Assays: Complications Arising from Ligand Depletion

S. Charlton, Juliet R. Leighton-Davies, Clare M Scaramellini Carter, 2007, Journal of biomolecular screening.

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

S. Briddon, S. Charlton, K. Gherbi, 2018, Scientific Reports.

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

S. Charlton, C. Brown, Michael R Boarder, 1997, British journal of pharmacology.

High Throughput Mutagenesis for Identification of Residues Regulating Human Prostacyclin (hIP) Receptor Expression and Function

A. Orth, L. Miraglia, Serge Batalov, 2014, PloS one.

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

H. Moore, J. R. Lane, J. Javitch, 2017, Nature Communications.

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

S. Charlton, G. Vauquelin, Georges Vauquelin, 2010, British journal of pharmacology.

Preassembled GPCR signaling complexes mediate distinct cellular responses to ultralow ligand concentrations

S. Charlton, O. Kleifeld, B. A. Evans, 2018, Science Signaling.

Kinetics of ligand binding and signaling

N. Holliday, S. Charlton, K. Sengmany, 2020 .

Single Step Determination of Unlabeled Compound Kinetics Using a Competition Association Binding Method Employing Time-Resolved FRET.

S. Charlton, D. Sykes, 2018, Methods in molecular biology.

Observed Drug-Receptor Association Rates Are Governed by Membrane Affinity: The Importance of Establishing “Micro-Pharmacokinetic/Pharmacodynamic Relationships” at the β2-Adrenoceptor

John Reilly, David A. Sykes, S. Charlton, 2014, Molecular Pharmacology.

The Antiallergic Mast Cell Stabilizers Lodoxamide and Bufrolin as the First High and Equipotent Agonists of Human and Rat GPR35

B. Hudson, G. Milligan, S. Nicklin, 2014, Molecular Pharmacology.

Microsoft Word-23820973-file00

B. Hudson, G. Milligan, Jennifer, 2013 .

Exploring the kinetic selectivity of antipsychotics for dopamine D2 and 5-HT2A receptors: implications for the prevalence of EPS and receptor occupancy

S. Charlton, D. Sykes, Palash Jain, 2021, bioRxiv.

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

S. Charlton, M. Loxham, P. Peachell, 2009 .

THEMED ISSUE: GPCR RESEARCH PAPER The long-acting b-adrenoceptor agonist, indacaterol, inhibits IgE-dependent responses of human lung mast cells

S. Charlton, M. Loxham, P. Peachell, 2009 .

Functional desensitization of the β2 adrenoceptor is not dependent on agonist efficacy

S. Charlton, M. Bradley, E. Rosethorne, 2015, Pharmacology research & perspectives.

Inhibition of the Proliferation of Human Lung Fibroblasts by Prostacyclin Receptor Agonists is Linked to a Sustained cAMP Signal in the Nucleus

L. May, S. Charlton, Maxine J. Roberts, 2021, Frontiers in Pharmacology.

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

S. Charlton, E. Rosethorne, 2018, Journal of experimental pharmacology.

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

S. Charlton, G. Vauquelin, Georges Vauquelin, 2010, British journal of pharmacology.

Measuring Receptor Target Coverage: A Radioligand Competition Binding Protocol for Assessing the Association and Dissociation Rates of Unlabeled Compounds

M. Dowling, S. Charlton, D. Sykes, 2010, Current protocols in pharmacology.

Kinetic Profiling of Ligands and Fragments Binding to GPCRs by TR-FRET

D. Veprintsev, S. Hill, S. Briddon, 2021, Biophysical and Computational Tools in Drug Discovery.

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

D. O'connor, S. Watson, S. Charlton, 2014, Bioorganic & medicinal chemistry letters.

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

J. Fozard, B. Cuenoud, S. Charlton, 2012, Bioorganic & medicinal chemistry letters.

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 β2 Adrenoceptor Agonist with a 24-h Duration of Action

J. Fozard, C. Battram, B. Cuenoud, 2006, Journal of Pharmacology and Experimental Therapeutics.

Agonist-Biased Signaling at the Histamine H4 Receptor: JNJ7777120 Recruits β-Arrestin without Activating G Proteins

S. Charlton, E. Rosethorne, 2011, Molecular Pharmacology.

Fentanyl binds to the μ-opioid receptor via the lipid membrane and transmembrane helices

R. Sessions, S. Charlton, R. Corey, 2021, bioRxiv.

M3-muscarinic receptor promotes insulin release via receptor phosphorylation/arrestin-dependent activation of protein kinase D1

J. Wess, A. Tobin, F. Hamdan, 2010, Proceedings of the National Academy of Sciences.

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

H. Moore, J. R. Lane, J. Javitch, 2017, Nature Communications.

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

J. Fozard, S. Charlton, M. Gosling, 2014, Bioorganic & medicinal chemistry letters.

The pharmacological rationale for combining muscarinic receptor antagonists and β-adrenoceptor agonists in the treatment of airway and bladder disease☆

M. Dowling, S. Charlton, M. Michel, 2014, Current opinion in pharmacology.

Reply to ‘Antipsychotics with similar association kinetics at dopamine D2 receptors differ in extrapyramidal side-effects’

J. R. Lane, J. Javitch, S. Charlton, 2018, Nature Communications.

Analysis of Multiple Histamine H4 Receptor Compound Classes Uncovers Gαi Protein- and β-Arrestin2-Biased Ligands

R. Leurs, H. Vischer, S. Charlton, 2012, Molecular Pharmacology.

ATP priming of macrophage-derived chemokine responses in CHO cells expressing the CCR4 receptor

David Beer, S. Charlton, David Beer, 2004, Naunyn-Schmiedeberg's Archives of Pharmacology.

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

S. Charlton, P. Aston, D. Sykes, 2015, British journal of pharmacology.

The Influence of Receptor Kinetics on the Onset and Duration of Action and the Therapeutic Index of NVA237 and Tiotropium

M. Dowling, S. Charlton, D. Sykes, 2012, Journal of Pharmacology and Experimental Therapeutics.

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

S. Charlton, D. Sykes, Kenny J. Watson, 2015, Toxicology and applied pharmacology.

signalling with ability to activate internalization

S. Charlton, C. Krasel, W. Dewey, 2010 .

Biased Agonism in Drug Discovery—Is It Too Soon to Choose a Path?

S. Charlton, M. Michel, 2018, Molecular Pharmacology.

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

S. Charlton, G. Vauquelin, 2013, British journal of pharmacology.

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

M. Dowling, S. Charlton, A. Sattikar, 2014, British journal of pharmacology.

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

S. Watson, S. Charlton, D. Sykes, 2016, Molecular Pharmacology.

Design, Synthesis, and Application of Fluorescent Ligands Targeting the Intracellular Allosteric Binding Site of the CXC Chemokine Receptor 2

Shailesh N Mistry, C. Laughton, N. Holliday, 2023, Journal of medicinal chemistry.

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

U. Schopfer, S. Charlton, D. Sykes, 2016, Journal of biomolecular screening.

The Influence of Receptor Kinetics on the Onset and Duration of Action and the Therapeutic Index of NVA237 and Tiotropium

M. Dowling, S. Charlton, D. Sykes, 2012, Journal of Pharmacology and Experimental Therapeutics.

BJP issue on drug discovery

S. Charlton, R. Bond, 2010, British journal of pharmacology.

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

S. Charlton, G. Vauquelin, 2010, British journal of pharmacology.

Detailed analysis of biased histamine H4 receptor signalling by JNJ 7777120 analogues

R. Leurs, H. Vischer, S. Charlton, 2013, British journal of pharmacology.

Design and synthesis of a library of chemokine antagonists.

T. Keller, S. Charlton, David Beer, 2011, Bioorganic & medicinal chemistry letters.