D. Sykes

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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 the kinetic selectivity of drugs targeting the β1‐adrenoceptor

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

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.

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.

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

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

Development of High-Specificity Fluorescent Probes to Enable Cannabinoid Type 2 Receptor Studies in Living Cells.

W. Guba, E. Carreira, A. Rufer, 2020, Journal of the American Chemical Society.

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.

Biased M1-muscarinic-receptor-mutant mice inform the design of next-generation drugs

P. Sexton, A. Christopoulos, S. Sakata, 2020, Nature Chemical Biology.

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.

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.

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

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

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.

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 .

Observed drug-receptor association rates are governed by membrane affinity: The importance of establishing “micro PK/PD relationships” at the 2 -adrenoceptor

D. Sykes, J. Reilly, R. A. Fairhurst, 2014 .

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.

Ligand Specific Efficiency (LSE) Index for PET Tracer Optimization

E. Briard, Y. Auberson, D. Sykes, 2016, ChemMedChem.

Optimization of the in vitro and in vivo properties of a novel series of 2,4,5-trisubstituted imidazoles as potent cholecystokinin-2 (CCK2) antagonists.

J. Black, C. Low, N. Shankley, 2005, Journal of medicinal chemistry.

Sonogashira/N-acyliminium ion aromatic π-cyclisation processes: access to tetra- and pentacyclic lactams

R. Grigg, D. Sykes, V. Sridharan, 2008 .

Discovery and characterization of novel, potent, non-peptide parathyroid hormone-1 receptor antagonists.

C. Low, C. Austin, D. Sykes, 2007, Journal of medicinal chemistry.

Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion.

J. Black, D. Sykes, I. Buck, 2007, Journal of medicinal chemistry.

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

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

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.

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.

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.

Binding kinetics of ligands acting at GPCRs

Leigh A. Stoddart, S. Hill, D. Sykes, 2019, Molecular and Cellular Endocrinology.

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.

GPCR Solubilization and Quality Control.

D. Veprintsev, D. Sykes, Tamara Miljuš, 2020, Methods in molecular biology.

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.

Functional solubilization of the β2-adrenoceptor using diisobutylene maleic acid

D. Veprintsev, S. Briddon, D. Poyner, 2021, iScience.

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.

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.

Combined docking and machine learning identify key molecular determinants of ligand pharmacological activity on β2 adrenoceptor

D. Veprintsev, E. Koers, D. Sykes, 2022, bioRxiv.

Functional solubilisation of the β2-adrenoceptor (β2AR) using Diisobutylene maleic acid (DIBMA)

D. Veprintsev, S. Briddon, D. Poyner, 2020, bioRxiv.

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.

ThermoFRET: A novel nanoscale G protein coupled receptor thermostability assay functional in crude solubilised membrane preparations

D. Veprintsev, D. Sykes, B. Hoare, 2020, bioRxiv.

Prediction of ligand-receptor pharmacological activities using a combined docking and machine learning approach

D. Veprintsev, E. Koers, D. Sykes, 2022 .

Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe

H. Spaink, W. Guba, E. Carreira, 2022, Chemical science.

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.

Platform Reagents Enable Synthesis of Ligand-Directed Covalent Probes: Study of Cannabinoid Receptor 2 in Live Cells.

W. Guba, E. Carreira, D. Veprintsev, 2023, Journal of the American Chemical Society.

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.

Development of a membrane-based Gi-CASE biosensor assay for profiling compounds at cannabinoid receptors

W. Guba, A. Rufer, D. Veprintsev, 2023, Frontiers in 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.

ThermoBRET: a ligand-engagement nanoscale thermostability assay applied to GPCRs

D. Veprintsev, N. Holliday, D. Sykes, 2020, bioRxiv.

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.

Ligand Specific Efficiency (LSE) Index for PET Tracer Optimization

E. Briard, Y. Auberson, D. Sykes, 2016, ChemMedChem.