Publications by authors named "David A Sykes"

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Water molecules in the cannabinoid receptor 2 binding site crucially impact the discovery of novel ligands.
Magdalena M Scharf, Morgan Scott-Dennis, Leire Borrega-Roman, Franziska N Z Giese, Darya Plevako, David A Sykes

Eur J Med Chem· December 2025

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Biased Signaling and Its Role in the Genesis of Short- and Long-Acting β-Adrenoceptor Agonists.
Ngan T N Phan, Leire Borrega-Roman, Bradley L Hoare, Clare R Harwood, Natalie Geary, David A Sykes

Biochemistry· August 2025

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Multiple intramolecular triggers converge to preferential G protein coupling in the CBR.
Adrian Morales-Pastor, Tamara Miljuš, Miguel Dieguez-Eceolaza, Tomasz Maciej Stępniewski, Vicente Ledesma-Martin, David A Sykes

Nat Commun· June 2025

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Profiling Allosteric Modulators of CBR with an Allosteric Fluoroprobe.
Miroslav Kosar, Themiya Perera, Rudolf L Z Ganzoni, Roman C Sarott, Leire Borrega-Roman, David A Sykes

Angew Chem Int Ed Engl· May 2025

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A universal cannabinoid CB1 and CB2 receptor TR-FRET kinetic ligand-binding assay.
Leire Borrega-Roman, Bradley L Hoare, Miroslav Kosar, Roman C Sarott, Kacper J Patej, David A Sykes

Front Pharmacol· April 2025

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Agonist efficacy at the βAR is driven by the faster association rate of the G protein.
Clare R Harwood, David A Sykes, Theo Redfern-Nichols, Owen Underwood, Colin Nicholson

Front Pharmacol· March 2025

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Structural basis of THC analog activity at the Cannabinoid 1 receptor.
Thor S Thorsen, Yashraj Kulkarni, David A Sykes, Andreas Bøggild, Taner Drace

Nat Commun· January 2025

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A Modified Cell-Penetrating Peptide Enhances Insulin and Oxytocin Delivery across an RPMI 2650 Nasal Epithelial Cell Barrier In Vitro.
Sara Wong, Alexander D Brown, Abigail B Abrahams, An Nisaa Nurzak, Hoda M Eltaher, David A Sykes

Pharmaceutics· September 2024

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Enhancing Drug Discovery and Development through the Integration of Medicinal Chemistry, Chemical Biology, and Academia-Industry Partnerships: Insights from Roche's Endocannabinoid System Projects.
Johannes Aebi, Kenneth Atz, Simon M Ametamey, Jörg Benz, Julie Blaising, David A Sykes

Chimia (Aarau)· August 2024

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Highly Selective Drug-Derived Fluorescent Probes for the Cannabinoid Receptor Type 1 (CBR).
Leonard Mach, Anahid Omran, Jara Bouma, Silke Radetzki, David A Sykes

J Med Chem· July 2024

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Flipping the GPCR Switch: Structure-Based Development of Selective Cannabinoid Receptor 2 Inverse Agonists.
Miroslav Kosar, Roman C Sarott, David A Sykes, Alexander E G Viray, Rosa Maria Vitale

ACS Cent Sci· May 2024

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ThermoBRET: A Ligand-Engagement Nanoscale Thermostability Assay Applied to GPCRs.
Bradley L Hoare, David N Tippett, Amandeep Kaur, Sean A Cullum, Tamara Miljuš, David A Sykes

Chembiochem· January 2024

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SmartWear body sensors for neurological and neurosurgical patients: A review of current and future technologies.
Nithin Gupta, Varun Kasula, Praveen Sanmugananthan, Nicholas Panico, Aimee H Dubin, David Aw Sykes

World Neurosurg X· January 2024

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Development of a membrane-based Gi-CASE biosensor assay for profiling compounds at cannabinoid receptors.
Morgan Scott-Dennis, Fikri A Rafani, Yicheng Yi, Themiya Perera, Clare R Harwood, David A Sykes

Front Pharmacol· August 2023

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Platform Reagents Enable Synthesis of Ligand-Directed Covalent Probes: Study of Cannabinoid Receptor 2 in Live Cells.
Miroslav Kosar, David A Sykes, Alexander E G Viray, Rosa Maria Vitale, Roman C Sarott

J Am Chem Soc· July 2023

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Combined docking and machine learning identify key molecular determinants of ligand pharmacological activity on β2 adrenoceptor.
Mireia Jiménez-Rosés, Bradley Angus Morgan, Maria Jimenez Sigstad, Thuy Duong Zoe Tran, Rohini Srivastava, David A Sykes

Pharmacol Res Perspect· October 2022

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Exploring the kinetic selectivity of drugs targeting the β -adrenoceptor.
David A Sykes, Mireia Jiménez-Rosés, John Reilly, Robin A Fairhurst, Steven J Charlton

Pharmacol Res Perspect· August 2022

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Functional solubilization of the β-adrenoceptor using diisobutylene maleic acid.
Clare R Harwood, David A Sykes, Bradley L Hoare, Franziska M Heydenreich, Romez Uddin

iScience· December 2021

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GPCR Solubilization and Quality Control.
Tamara Miljus, David A Sykes, Clare R Harwood, Ziva Vuckovic, Dmitry B Veprintsev

Methods Mol Biol· March 2021

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Development of High-Specificity Fluorescent Probes to Enable Cannabinoid Type 2 Receptor Studies in Living Cells.
Roman C Sarott, Matthias V Westphal, Patrick Pfaff, Claudia Korn, David A Sykes

J Am Chem Soc· October 2020

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Biased M1-muscarinic-receptor-mutant mice inform the design of next-generation drugs.
Sophie J Bradley, Colin Molloy, Paulina Valuskova, Louis Dwomoh, Miriam Scarpa, David A Sykes

Nat Chem Biol· March 2020

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Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D Receptor.
Tim J Fyfe, Barrie Kellam, David A Sykes, Ben Capuano, Peter J Scammells

J Med Chem· November 2019

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VEGFA From Early Osteoblast Lineage Cells (Osterix+) Is Required in Mice for Fracture Healing.
Evan G Buettmann, Jennifer A McKenzie, Nicole Migotsky, David Aw Sykes, Pei Hu

J Bone Miner Res· September 2019

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Investigating the Influence of Tracer Kinetics on Competition-Kinetic Association Binding Assays: Identifying the Optimal Conditions for Assessing the Kinetics of Low-Affinity Compounds.
David A Sykes, Palash Jain, Steven J Charlton

Mol Pharmacol· September 2019

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Pharmacological Characterization of a Novel 5-Hydroxybenzothiazolone-Derived -Adrenoceptor Agonist with Functional Selectivity for Anabolic Effects on Skeletal Muscle Resulting in a Wider Cardiovascular Safety Window in Preclinical Studies.
Magdalena Koziczak-Holbro, Dean F Rigel, Bérengère Dumotier, David A Sykes, Jeffrey Tsao

J Pharmacol Exp Ther· May 2019

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