Stephen J Hill

Scopus Publications

Two-Step Ligand-Directed Covalent Fluorescent Labeling of the Adenosine A1-Receptor That Maintains Its Orthosteric Binding Site’s Availability to Bind Ligands
Chia-Yang Lin, Simon Platt, Joelle Goulding, Stephen J. Briddon, Nicholas D. Kindon, Clare R. Harwood, Chih-Wei Lai, Barrie Kellam, Stephen J. Hill
Journal of Medicinal Chemistry, 2026
receptor using click chemistry. We also describe a range of biophysical approaches to confirm that the orthosteric binding site remains available to interact with endogenous ligands, agonists and antagonists, and access to the orthosteric binding site is not sterically hindered by the transferred cargo (fluorophore or click-reactive group).
Cannabinoid CB2 receptor drives trastuzumab resistance and predicts durable anti-HER2 response
Marta Seijo-Vila, Sofía A. Balsinde, Sandra Blasco-Benito, Isabel Tundidor, María Rubert-Hernández, Ana Montero-Calle, Rodrigo Barderas, Laura E. Kilpatrick, Simon Platt, Noemi Karsai, Isabel Philps, Olga M. Antón, Déborah Gómez-Domínguez, Ignacio Pérez de Castro, Carmen González-Lois, Diego García-Fresnadillo, Gala Silvestre-Egea, Antonio J. Sánchez-López, Esther Ramírez-Medina, María Catalina Rivas Prieto, Belén Almoguera Pérez-Cejuela, Luis Manso, Sandra Zazo, Noemí López-Ejeda, Francisco Palomino-Duque, María Turienzo-Durán, Nuria G. Martínez-Illescas, María Salazar-Roa, Sonia Castillo-Lluva, Stephen J. Hill, Manuel Guzmán, Eduardo Pérez-Gómez, Cristina Sánchez
Oncogene, 2026
Acquired or innate lack of response to standard HER2-targeted therapies remains a clinical issue in patients with HER2-positive breast cancer. Here, we investigated the role of the cannabinoid CB 2 receptor (CB 2 R) in trastuzumab resistance. In human breast cancer samples, a decreased expression of HER2-CB 2 R heterodimers following neoadjuvant treatment, due to CB 2 R downregulation, was linked to poor long-term outcomes. Using various preclinical models, we demonstrate that CB 2 R drives trastuzumab resistance. Mechanistically, CB 2 R loss enabled cancer cells to evade antitumor IFN-γ signaling while promoting a shift from HER2-CB 2 R to HER2-EGFR heterodimers, thus reducing dependence on HER2 and increasing reliance on EGFR-mediated pathways. Moreover, EGFR inhibition restored trastuzumab sensitivity. In summary, we reveal an unprecedented role for CB 2 R as a key regulator of oncogenic and immune signaling in response to anti-HER2 therapy and its potential as a predictive biomarker of therapeutic efficacy. We also propose dual HER2/EGFR targeting and non-CB 2 R-selective cannabinoid therapies as potential strategies to overcome CB 2 R-mediated trastuzumab resistance. Together, these findings position the endocannabinoid system as a pivotal and actionable node to elucidate, anticipate, and counteract resistance to HER2-targeted therapies.
Acute vascular and cardiac effects of lenvatinib in mice
Dustin N. Krüger, Patrizia Pannucci, Callan D. Wesley, Cedric H. G. Neutel, Wim Martinet, Guido R. Y. De Meyer, Stephen J. Hill, Jeanette Woolard, Constantijn Franssen, Pieter-Jan Guns
Cardio Oncology, 2025
BACKGROUND: Tyrosine kinase inhibitors (TKIs) targeting vascular endothelial growth factor (VEGF) receptor signalling are used in cancer therapy to inhibit angiogenesis. Unfortunately, VEGF inhibitors are known to induce severe hypertension in patients. This study aimed to elucidate the impact of the TKI lenvatinib on blood pressure, arterial stiffness, vascular reactivity, as well as cardiac function in a short-term murine model to shed light on potential contributors to cardiovascular (CV) toxicities associated with VEGF inhibition. METHODS: Male C57BL/6J mice were randomly divided into 2 cohorts, either treated for 4 days with lenvatinib 4 mg/kg/day or 40% hydroxypropyl β-cyclodextrin as control. In an additional study, mice were subjected to a 4-day treatment followed by a 4-day wash-out, with echocardiography and blood pressure measurements performed on day 2 and 7. Subsequently, ex vivo vascular reactivity of thoracic aortic segments was determined. RESULTS: Lenvatinib induced hypertension and arterial stiffness (i.e., increased pulse wave velocity), starting from day 2 of treatment. Further, left ventricular ejection fraction was reduced and the ventricle dilated upon treatment. Lenvatinib induced neither endothelial dysfunction nor impaired vascular smooth muscle cell reactivity to nitric oxide (NO). Interestingly, lenvatinib demonstrated a concentration-dependent increase in ATP-mediated relaxation. In addition, after the 4-day wash-out period, lenvatinib-treated mice did not show complete remission of hypertension. However, arterial stiffness, ATP-mediated relaxation and cardiac adaptation were recovered. CONCLUSION: This comprehensive investigation provides valuable insights into the interplay between VEGF inhibition, vascular function and cardiac outcomes, emphasising the need for nuanced understanding and further exploration of the differential effects of lenvatinib on the CV system. Additionally, the study proposes a synergistic formation between VEGF and ATP, indicating an enhanced response via P2Yx receptor signalling.
Quantitative analysis of human umbilical vein endothelial cell morphology and tubulogenesis
Viviane Mignone, Maria Augusta Arruda, Laura Kilpatrick, Benjamin Moore, Jeanette Woolard, Stephen Hill, Joëlle Goulding
Journal of Microscopy, 2025
Primary human umbilical vein endothelial cells can grow as both a monolayer in culture and also as a capillary‐like network making them an ideal model system in order to study vascular remodelling. Image‐based analysis can allow assessment of cell morphology and motility but is dependent on accurate cell segmentation which requires high‐contrast images not normally achievable without fluorescent markers. Here, ptychography is employed as a label‐free image‐based modality in order to extract quantitative metrics of morphology and tubulogenesis from cultured HUVECs over time in an automated multiwell assay. Phase‐specific parameters of dry mass, optical thickness and sphericity were extracted and assessed alongside other metrics of cell number and shape. Tubulogenesis could be captured dynamically without any imaging artefacts from use of a basement membrane matrix and metrics of tube number, growth and branching exported alongside morphology metrics at early time‐points. Utilising ptychography‐based image analysis, all VEGF165a isoforms studied, elicited a concentration‐dependent effect on cell elongation and survival within a HUVEC monolayer. Pharmacologically relevant parameters of potency (EC50) and efficacy were derived, exemplifying this label‐free approach for the multiparameter and multiwell quantitative study of vascular remodelling in physiologically relevant cells at 37°C.
Mechano-sensitivity of β2-adrenoceptors enhances constitutive activation of cAMP generation that is inhibited by inverse agonists
Sean A. Cullum, Simon Platt, Natasha Dale, Oliver C. Isaac, Edward S. Wragg, Mark Soave, Dmitry B. Veprintsev, Jeanette Woolard, Laura E. Kilpatrick, Stephen J. Hill
Communications Biology, 2024
The concept of agonist-independent signalling that can be attenuated by inverse agonists is a fundamental element of the cubic ternary complex model of G protein-coupled receptor (GPCR) activation. This model shows how a GPCR can exist in two conformational states in the absence of ligands; an inactive R state and an active R* state that differ in their affinities for agonists, inverse agonists, and G-protein alpha subunits. The proportion of R* receptors that exist in the absence of agonists determines the level of constitutive receptor activity. In this study we demonstrate that mechanical stimulation can induce β2-adrenoceptor agonist-independent Gs-mediated cAMP signalling that is sensitive to inhibition by inverse agonists such as ICI-118551 and propranolol. The size of the mechano-sensitive response is dependent on the cell surface receptor expression level in HEK293G cells, is still observed in a ligand-binding deficient D113A mutant β2-adrenoceptor and can be attenuated by site-directed mutagenesis of the extracellular N-glycosylation sites on the N-terminus and second extracellular loop of the β2-adrenoceptor. Similar mechano-sensitive agonist-independent responses are observed in HEK293G cells overexpressing the A2A-adenosine receptor. These data provide new insights into how agonist-independent constitutive receptor activity can be enhanced by mechanical stimulation and regulated by inverse agonists.
Kinetic analysis of fluorescent ligand binding to cell surface receptors: Insights into conformational changes and allosterism in living cells
Stephen J. Hill, Laura E. Kilpatrick
British Journal of Pharmacology, 2024
Equilibrium binding assays are one of the mainstays of current drug discovery efforts to evaluate the interaction of drugs with receptors in membranes and intact cells. However, in recent years, there has been increased focus on the kinetics of the drug–receptor interaction to gain insight into the lifetime of drug–receptor complexes and the rate of association of a ligand with its receptor. Furthermore, drugs that act on topically distinct sites (allosteric) from those occupied by the endogenous ligand (orthosteric site) can induce conformational changes in the orthosteric binding site leading to changes in the association and/or dissociation rate constants of orthosteric ligands. Conformational changes in the orthosteric ligand binding site can also be induced through interaction with neighbouring accessory proteins and receptor homodimerisation and heterodimerisation. In this review, we provide an overview of the use of fluorescent ligand technologies to interrogate ligand–receptor kinetics in living cells and the novel insights that they can provide into the conformational changes induced by drugs acting on a variety of cell surface receptors including G protein‐coupled receptors (GPCRs), receptor tyrosine kinases (RTKs) and cytokine receptors.
Role of endothelin ETA receptors in the hypertension induced by the VEGFR-2 kinase inhibitors axitinib and lenvatinib in conscious freely-moving rats
Patrizia Pannucci, Marieke Van Daele, Samantha L. Cooper, Edward S. Wragg, Julie March, Marleen Groenen, Stephen J. Hill, Jeanette Woolard
Biochemical Pharmacology, 2024
Receptor tyrosine kinase inhibitors (RTKIs) suppress tumour growth by targeting vascular endothelial growth factor receptor 2 (VEGFR-2) which is an important mediator of angiogenesis. Here, we demonstrate that two potent RTKIs, axitinib and lenvatinib, are associated with hypertensive side effects. Doppler flowmetry was used to evaluate regional haemodynamic profiles of axitinib and lenvatinib. Male Sprague Dawley rats (350–500 g) were instrumented with Doppler flow probes (renal and mesenteric arteries and descending abdominal aorta) and catheters (jugular vein and distal abdominal aorta, via the caudal artery). Rats were dosed daily with axitinib (3 or 6 mg.kg−1) or lenvatinib (1 or 3 mg.kg−1) and regional haemodynamics were recorded over a maximum of 4 days. Both RTKIs caused significant (p < 0.05) increases in mean arterial pressure (MAP), which was accompanied by significant (p < 0.05) vasoconstriction in both the mesenteric and hindquarters vascular beds. To gain insight into the involvement of endothelin-1 (ET-1) in RTKI-mediated hypertension, we also monitored heart rate (HR) and MAP in response to axitinib or lenvatinib in animals treated with the ETA receptor selective antagonist sitaxentan (5 mg.kg−1) or the mixed ETA/ETB receptor antagonist bosentan (15 mg.kg−1) over two days. Co-treatment with bosentan or sitaxentan markedly reduced the MAP effects mediated by both RTKIs (p < 0.05). Bosentan, but not sitaxentan, also attenuated ET-1 mediated increases in HR. These data suggest that selective antagonists of ETA receptors may be appropriate to alleviate the hypertensive effects of axitinib and lenvatinib.
A novel and selective fluorescent ligand for the study of adenosine A2B receptors
Foteini Patera, Sarah J. Mistry, Nicholas D. Kindon, Eleonora Comeo, Joelle Goulding, Barrie Kellam, Laura E. Kilpatrick, Hester Franks, Stephen J. Hill
Pharmacology Research and Perspectives, 2024
Fluorescent ligands have proved to be powerful tools in the study of G protein‐coupled receptors in living cells. Here we have characterized a new fluorescent ligand PSB603‐BY630 that has high selectivity for the human adenosine A2B receptor (A2BR). The A2BR appears to play an important role in regulating immune responses in the tumor microenvironment. Here we have used PSB603‐BY630 to monitor specific binding to A2BRs in M1‐ and M2‐like macrophages derived from CD14+ human monocytes. PSB603‐BY630 bound with high affinity (18.3 nM) to nanoluciferase‐tagged A2BRs stably expressed in HEK293G cells. The ligand exhibited very high selectivity for the A2BR with negligible specific‐binding detected at NLuc‐A2AR, NLuc‐A1R, or NLuc‐A3R receptors at concentrations up to 500 nM. Competition binding studies showed the expected pharmacology at A2BR with the A2BR‐selective ligands PSB603 and MRS‐1706 demonstrating potent inhibition of the specific binding of 50 nM PSB603‐BY630 to A2BR. Functional studies in HEK293G cells using Glosensor to monitor Gs‐coupled cyclic AMP responses indicated that PSB603‐BY630 acted as a negative allosteric regular of the agonist responses to BAY 60–6583. Furthermore, flow cytometry analysis confirmed that PSB603‐BY630 could be used to selectively label endogenous A2BRs expressed on human macrophages. This ligand should be an important addition to the library of fluorescent ligands which are selective for the different adenosine receptor subtypes, and will enable study of the role of A2BRs on immune cells in the tumor microenvironment.
Ligand-Directed Labeling of the Adenosine A1 Receptor in Living Cells
Eleonora Comeo, Joëlle Goulding, Chia-Yang Lin, Marleen Groenen, Jeanette Woolard, Nicholas D. Kindon, Clare R. Harwood, Simon Platt, Stephen J. Briddon, Laura E. Kilpatrick, Peter J. Scammells, Stephen J. Hill, Barrie Kellam
Journal of Medicinal Chemistry, 2024
The study of protein function and dynamics in their native cellular environment is essential for progressing fundamental science. To overcome the requirement of genetic modification of the protein or the limitations of dissociable fluorescent ligands, ligand-directed (LD) chemistry has most recently emerged as a complementary, bioorthogonal approach for labeling native proteins. Here, we describe the rational design, development, and application of the first ligand-directed chemistry approach for labeling the A1AR in living cells. We pharmacologically demonstrate covalent labeling of A1AR expressed in living cells while the orthosteric binding site remains available. The probes were imaged using confocal microscopy and fluorescence correlation spectroscopy to study A1AR localization and dynamics in living cells. Additionally, the probes allowed visualization of the specific localization of A1ARs endogenously expressed in dorsal root ganglion (DRG) neurons. LD probes developed here hold promise for illuminating ligand-binding, receptor signaling, and trafficking of the A1AR in more physiologically relevant environments.
Design, Synthesis, and Evaluation of a New Chemotype Fluorescent Ligand for the P2Y2 Receptor
Rebecca Knight, Laura E. Kilpatrick, Stephen J. Hill, Michael J. Stocks
ACS Medicinal Chemistry Letters, 2024
The P2Y2 receptor (P2Y2R) is a target for diseases including cancer, idiopathic pulmonary fibrosis, and atherosclerosis. However, there are insufficient P2Y2R antagonists available for validating P2Y2R function and future drug development. Evaluation of how (R)-5-(7-chloro-2-((2-ethoxyethyl)amino)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-1-methyl-4-thioxo-3,4-dihydropyrimidin-2(1H)-one, a previously published thiazole-based analogue of AR-C118925, binds in a P2Y2R homology model was used to design new P2Y2R antagonist scaffolds. One P2Y2R antagonist scaffold retained millimolar affinity for the P2Y2R and upon further functionalization with terminal carboxylic acid groups affinity was improved over 100-fold. This functionalized P2Y2R antagonist scaffold was employed to develop new chemotype P2Y2R fluorescent ligands, that were attainable in a convergent five-step synthesis. One of these fluorescent ligands demonstrated micromolar affinity (pKd = 6.02 ± 0.12, n = 5) for the P2Y2R in isolated cell membranes and distinct pharmacology from an existing P2Y2R fluorescent antagonist, suggesting it may occupy a different binding site on the P2Y2R.
CXCL17 is an allosteric inhibitor of CXCR4 through a mechanism of action involving glycosaminoglycans
Carl W. White, Simon Platt, Laura E. Kilpatrick, Natasha Dale, Rekhati S. Abhayawardana, Sebastian Dekkers, Nicholas D. Kindon, Barrie Kellam, Michael J. Stocks, Kevin D. G. Pfleger, Stephen J. Hill
Science Signaling, 2024
Small Molecule Fluorescent Ligands for the Atypical Chemokine Receptor 3 (ACKR3)
Sebastian Dekkers, Dehan Comez, Noemi Karsai, Marta Arimont-Segura, Meritxell Canals, Birgit Caspar, Chris de Graaf, Laura E. Kilpatrick, Rob Leurs, Barrie Kellam, Stephen J. Hill, Stephen J. Briddon, Michael J. Stocks
ACS Medicinal Chemistry Letters, 2024
Characterisation of IL-23 receptor antagonists and disease relevant mutants using fluorescent probes
Charles S. Lay, Albert Isidro-Llobet, Laura E. Kilpatrick, Peter D. Craggs, Stephen J. Hill
Nature Communications, 2023
Characterisation of tyrosine kinase inhibitor-receptor interactions at VEGFR2 using sunitinib-red and nanoBRET
Marieke Van Daele, Laura E. Kilpatrick, Jeanette Woolard, Stephen J. Hill
Biochemical Pharmacology, 2023
Probing expression of E-selectin using CRISPR-Cas9-mediated tagging with HiBiT in human endothelial cells
Lydia Ogrodzinski, Simon Platt, Joelle Goulding, Cameron Alexander, Tracy D. Farr, Jeanette Woolard, Stephen J. Hill, Laura E. Kilpatrick
Iscience, 2023
Use of NanoBiT and NanoBRET to characterise interleukin-23 receptor dimer formation in living cells
Charles S. Lay, Laura E. Kilpatrick, Peter D. Craggs, Stephen J. Hill
British Journal of Pharmacology, 2023
Plasma membrane preassociation drives β-arrestin coupling to receptors and activation
Jak Grimes, Zsombor Koszegi, Yann Lanoiselée, Tamara Miljus, Shannon L. O’Brien, Tomasz M. Stepniewski, Brian Medel-Lacruz, Mithu Baidya, Maria Makarova, Ravi Mistry, Joëlle Goulding, Julia Drube, Carsten Hoffmann, Dylan M. Owen, Arun K. Shukla, Jana Selent, Stephen J. Hill, Davide Calebiro
Cell, 2023
Kinetic analysis of endogenous β2-adrenoceptor-mediated cAMP GloSensor™ responses in HEK293 cells
Sean A. Cullum, Dmitry B. Veprintsev, Stephen J. Hill
British Journal of Pharmacology, 2023
Small-Molecule Fluorescent Ligands for the CXCR4 Chemokine Receptor
Sebastian Dekkers, Birgit Caspar, Joëlle Goulding, Nicholas D. Kindon, Laura E. Kilpatrick, Leigh A. Stoddart, Stephen J. Briddon, Barrie Kellam, Stephen J. Hill, Michael J. Stocks
Journal of Medicinal Chemistry, 2023
NanoB2 to monitor interactions of ligands with membrane proteins by combining nanobodies and NanoBRET
Jelle van den Bor, Nick D. Bergkamp, Stephanie M. Anbuhl, Françoise Dekker, Dehan Comez, Claudia V. Perez Almeria, Reggie Bosma, Carl W. White, Laura E. Kilpatrick, Stephen J. Hill, Marco Siderius, Martine J. Smit, Raimond Heukers
Cell Reports Methods, 2023
COVID-19-Induced Myocarditis: Pathophysiological Roles of ACE2 and Toll-like Receptors
Patrizia Pannucci, Sophie R. Jefferson, Jonathan Hampshire, Samantha L. Cooper, Stephen J. Hill, Jeanette Woolard
International Journal of Molecular Sciences, 2023
Fluorescently tagged nanobodies and NanoBRET to study ligand-binding and agonist-induced conformational changes of full-length EGFR expressed in living cells
Dehan Comez, Jacqueline Glenn, Stephanie M. Anbuhl, Raimond Heukers, Martine J. Smit, Stephen J. Hill, Laura E. Kilpatrick
Frontiers in Immunology, 2022
Community guidelines for GPCR ligand bias: IUPHAR review 32
Peter Kolb, Terry Kenakin, Stephen P. H. Alexander, Marcel Bermudez, Laura M. Bohn, Christian S. Breinholt, Michel Bouvier, Stephen J. Hill, Evi Kostenis, Kirill A. Martemyanov, Rick R. Neubig, H. Ongun Onaran, Sudarshan Rajagopal, Bryan L. Roth, Jana Selent, Arun K. Shukla, Martha E. Sommer, David E. Gloriam
British Journal of Pharmacology, 2022
Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H1Receptor
Zhi Yuan Kok, Leigh A. Stoddart, Sarah J. Mistry, Tamara A. M. Mocking, Henry F. Vischer, Rob Leurs, Stephen J. Hill, Shailesh N. Mistry, Barrie Kellam
Journal of Medicinal Chemistry, 2022
Involvement of β-adrenoceptors in the cardiovascular responses induced by selective adenosine A2A and A2B receptor agonists
Edward S. Wragg, Patrizia Pannucci, Stephen J. Hill, Jeanette Woolard, Samantha L. Cooper
Pharmacology Research and Perspectives, 2022
Regionally selective cardiovascular responses to adenosine A2A and A2B receptor activation
Samantha L. Cooper, Edward S. Wragg, Patrizia Pannucci, Mark Soave, Stephen J. Hill, Jeanette Woolard
FASEB Journal, 2022
Probing the binding of interleukin-23 to individual receptor components and the IL-23 heteromeric receptor complex in living cells using NanoBRET
Charles S. Lay, Angela Bridges, Joelle Goulding, Stephen J. Briddon, Zoja Soloviev, Peter D. Craggs, Stephen J. Hill
Cell Chemical Biology, 2022
Evidence that GPVI is Expressed as a Mixture of Monomers and Dimers, and that the D2 Domain is not Essential for GPVI Activation
Joanne C. Clark, Raluca A. I. Neagoe, Malou Zuidscherwoude, Deirdre M. Kavanagh, Alexandre Slater, Eleyna M. Martin, Mark Soave, David Stegner, Bernhard Nieswandt, Natalie S. Poulter, Johan Hummert, Dirk-Peter Herten, Michael G. Tomlinson, Stephen J. Hill, Steve P. Watson
Thrombosis and Haemostasis, 2021
The use of fluorescence correlation spectroscopy to characterise the molecular mobility of G proteincoupled receptors in membrane microdomains: An update
Laura E. Kilpatrick, Stephen J. Hill
Biochemical Society Transactions, 2021
Role of the renin–angiotensin–aldosterone and kinin–kallikrein systems in the cardiovascular complications of COVID-19 and long COVID
Samantha L. Cooper, Eleanor Boyle, Sophie R. Jefferson, Calum R. A. Heslop, Pirathini Mohan, Gearry G. J. Mohanraj, Hamza A. Sidow, Rory C. P. Tan, Stephen J. Hill, Jeanette Woolard
International Journal of Molecular Sciences, 2021
Development of Covalent, Clickable Probes for Adenosine A1and A3Receptors
Phuc N. H. Trinh, Daniel J. W. Chong, Katie Leach, Stephen J. Hill, Joel D. A. Tyndall, Lauren T. May, Andrea J. Vernall, Karen J. Gregory
Journal of Medicinal Chemistry, 2021
Use of NanoBiT and NanoBRET to monitor fluorescent VEGF-A binding kinetics to VEGFR2/NRP1 heteromeric complexes in living cells
Chloe J. Peach, Laura E. Kilpatrick, Jeanette Woolard, Stephen J. Hill
British Journal of Pharmacology, 2021
Development and Application of Subtype-Selective Fluorescent Antagonists for the Study of the Human Adenosine A1Receptor in Living Cells
Eleonora Comeo, Phuc Trinh, Anh T. Nguyen, Cameron J. Nowell, Nicholas D. Kindon, Mark Soave, Leigh A. Stoddart, Jonathan M. White, Stephen J. Hill, Barrie Kellam, Michelle L. Halls, Lauren T. May, Peter J. Scammells
Journal of Medicinal Chemistry, 2021
Subtype selective fluorescent ligands based on ICI 118,551 to study the human β2-adrenoceptor in CRISPR/Cas9 genome-edited HEK293T cells at low expression levels
Joëlle Goulding, Sarah J. Mistry, Mark Soave, Jeanette Woolard, Stephen J. Briddon, Carl W. White, Barrie Kellam, Stephen J. Hill
Pharmacology Research and Perspectives, 2021
Efficient G protein coupling is not required for agonist-mediated internalization and membrane reorganization of the adenosine A3 receptor
Leigh A. Stoddart, Laura E. Kilpatrick, Ross Corriden, Barrie Kellam, Stephen J. Briddon, Stephen J. Hill
FASEB Journal, 2021
Detection of genome-edited and endogenously expressed G protein-coupled receptors
Mark Soave, Leigh A. Stoddart, Carl W. White, Laura E. Kilpatrick, Joëlle Goulding, Stephen J. Briddon, Stephen J. Hill
FEBS Journal, 2021
The use of fluorescence correlation spectroscopy to monitor cell surface β2-adrenoceptors at low expression levels in human embryonic stem cell-derived cardiomyocytes and fibroblasts
Joëlle Goulding, Alexander Kondrashov, Sarah J. Mistry, Tony Melarangi, Nguyen T.N. Vo, Duc M. Hoang, Carl W. White, Chris Denning, Stephen J. Briddon, Stephen J. Hill
FASEB Journal, 2021
CRISPR/Cas9-mediated generation and analysis of N terminus polymorphic models of β2AR in isogenic hPSC-derived cardiomyocytes
Alexander Kondrashov, Nurul A.N. Mohd Yusof, Alveera Hasan, Joëlle Goulding, Thusharika Kodagoda, Duc M. Hoang, Nguyen T.N. Vo, Tony Melarangi, Nazanin Dolatshad, Julia Gorelik, Stephen J. Hill, Sian E. Harding, Chris Denning
Molecular Therapy Methods and Clinical Development, 2021
Transactivation of G protein-coupled receptors (GPCRs) and receptor tyrosine kinases (RTKs): Recent insights using luminescence and fluorescence technologies
Laura E. Kilpatrick, Stephen J. Hill
Current Opinion in Endocrine and Metabolic Research, 2021
Article investigation of receptor heteromers using nanobret ligand binding
Elizabeth K. M. Johnstone, Heng B. See, Rekhati S. Abhayawardana, Angela Song, K. Johan Rosengren, Stephen J. Hill, Kevin D. G. Pfleger
International Journal of Molecular Sciences, 2021
A nanoluciferase biosensor to investigate endogenous chemokine secretion and receptor binding
Carl W. White, Laura E. Kilpatrick, Kevin D.G. Pfleger, Stephen J. Hill
Iscience, 2021
Kinetic Profiling of Ligands and Fragments Binding to GPCRs by TR-FRET
David A. Sykes, Leire Borrega-Roman, Clare R. Harwood, Bradley Hoare, Jack M. Lochray, Thais Gazzi, Stephen J. Briddon, Marc Nazaré, Uwe Grether, Stephen J. Hill, Steven J. Charlton, Dmitry B. Veprintsev
Topics in Medicinal Chemistry, 2021
A lipid-anchored neurokinin 1 receptor antagonist prolongs pain relief by a three-pronged mechanism of action targeting the receptor at the plasma membrane and in endosomes
Quynh N. Mai, Priyank Shenoy, Tim Quach, Jeffri S. Retamal, Arisbel B. Gondin, Holly R. Yeatman, Luigi Aurelio, Joshua W. Conner, Daniel P. Poole, Meritxell Canals, Cameron J. Nowell, Bim Graham, Thomas P. Davis, Stephen J. Briddon, Stephen J. Hill, Christopher J.H. Porter, Nigel W. Bunnett, Michelle L. Halls, Nicholas A. Veldhuis
Journal of Biological Chemistry, 2021
Ligand-directed covalent labelling of a GPCR with a fluorescent tag in live cells
Leigh A. Stoddart, Nicholas D. Kindon, Omolade Otun, Clare R. Harwood, Foteini Patera, Dmitry B. Veprintsev, Jeanette Woolard, Stephen J. Briddon, Hester A. Franks, Stephen J. Hill, Barrie Kellam
Communications Biology, 2020
Monitoring Allosteric Interactions with CXCR4 Using NanoBiT Conjugated Nanobodies
Mark Soave, Raimond Heukers, Barrie Kellam, Jeanette Woolard, Martine J. Smit, Stephen J. Briddon, Stephen J. Hill
Cell Chemical Biology, 2020
Using Esterase Selectivity to Determine the in Vivo Duration of Systemic Availability and Abolish Systemic Side Effects of Topical β-Blockers
Jillian G. Baker, Christophe Fromont, Marjorie Bruder, Kevin S. J. Thompson, Barrie Kellam, Stephen J. Hill, Sheila M. Gardiner, Peter M. Fischer
ACS Pharmacology and Translational Science, 2020
Kinetic analysis of the early signaling steps of the human chemokine receptor CXCR4
Cristina Perpiñá-Viciano, Ali Işbilir, Aurélien Zarca, Birgit Caspar, Laura E. Kilpatrick, Stephen J. Hill, Martine J. Smit, Martin J. Lohse, Carsten Hoffmann
Molecular Pharmacology, 2020
Quantifying Target Occupancy of Small Molecules within Living Cells
M.B. Robers, R. Friedman-Ohana, K.V.M. Huber, L. Kilpatrick, J.D. Vasta, B.-T. Berger, C. Chaudhry, S. Hill, S. Müller, S. Knapp, K.V. Wood
Annual Review of Biochemistry, 2020
Single molecule binding of a ligand to a G-protein-coupled receptor in real time using fluorescence correlation spectroscopy, rendered possible by nano-encapsulation in styrene maleic acid lipid particles
Rachael L. Grime, Joelle Goulding, Romez Uddin, Leigh A. Stoddart, Stephen J. Hill, David R. Poyner, Stephen J. Briddon, Mark Wheatley
Nanoscale, 2020
CRISPR-Mediated Protein Tagging with Nanoluciferase to Investigate Native Chemokine Receptor Function and Conformational Changes
Carl W. White, Birgit Caspar, Hannah K. Vanyai, Kevin D.G. Pfleger, Stephen J. Hill
Cell Chemical Biology, 2020
Subtype-Selective Fluorescent Ligands as Pharmacological Research Tools for the Human Adenosine A2A Receptor
Eleonora Comeo, Nicholas D. Kindon, Mark Soave, Leigh A. Stoddart, Laura E. Kilpatrick, Peter J. Scammells, Stephen J. Hill, Barrie Kellam
Journal of Medicinal Chemistry, 2020
Fluorescent ligands: Bringing light to emerging GPCR paradigms
Mark Soave, Stephen J. Briddon, Stephen J. Hill, Leigh A. Stoddart
British Journal of Pharmacology, 2020
NanoBiT Complementation to Monitor Agonist-Induced Adenosine A1 Receptor Internalization
Mark Soave, Barrie Kellam, Jeanette Woolard, Stephen J. Briddon, Stephen J. Hill
Slas Discovery, 2020
Application of fluorescent purinoceptor antagonists for bioluminescence resonance energy transfer assays and fluorescent microscopy
Mark Soave, Joëlle Goulding, Robert Markus, Stephen J. Hill, Leigh A. Stoddart
Methods in Molecular Biology, 2020
The effect of two selective A1-receptor agonists and the bitopic ligand VCP746 on heart rate and regional vascular conductance in conscious rats
Samantha L. Cooper, Julie March, Andrea R. Sabbatini, Stephen J. Hill, Manuela Jörg, Peter J. Scammells, Jeanette Woolard
British Journal of Pharmacology, 2020
CXCR4/AckR3 phosphorylation and recruitment of interacting proteins: Key mechanisms regulating their functional status
Amos Fumagalli, Aurélien Zarca, Maria Neves, Birgit Caspar, Stephen J. Hill, Federico Mayor Jr., Martine J. Smit, Philippe Marin
Molecular Pharmacology, 2019
Optimised insert design for improved single-molecule imaging and quantification through CRISPR-Cas9 mediated knock-in
Abdullah O. Khan, Carl W. White, Jeremy A. Pike, Jack Yule, Alexandre Slater, Stephen J. Hill, Natalie S. Poulter, Steven G. Thomas, Neil V. Morgan
Scientific Reports, 2019
Context-dependent signaling of CXC chemokine receptor 4 and atypical chemokine receptor 3
Joyce Heuninck, Cristina Perpiñá Viciano, Ali Işbilir, Birgit Caspar, Davide Capoferri, Stephen J. Briddon, Thierry Durroux, Stephen J. Hill, Martin J. Lohse, Graeme Milligan, Jean-Philippe Pin, Carsten Hoffmann
Molecular Pharmacology, 2019
Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor
Reggie Bosma, Leigh A. Stoddart, Victoria Georgi, Monica Bouzo-Lorenzo, Nick Bushby, Loretta Inkoom, Michael J. Waring, Stephen J. Briddon, Henry F. Vischer, Robert J. Sheppard, Amaury Fernández-Montalván, Stephen J. Hill, Rob Leurs
Scientific Reports, 2019
Modulators of CXCR4 and CXCR7/AckR3 function
Ilze Adlere, Birgit Caspar, Marta Arimont, Sebastian Dekkers, Kirsten Visser, Jeffrey Stuijt, Chris de Graaf, Michael Stocks, Barrie Kellam, Stephen Briddon, Maikel Wijtmans, Iwan de Esch, Stephen Hill, Rob Leurs
Molecular Pharmacology, 2019
Complex Formation between VEGFR2 and the β2-Adrenoceptor
Laura E. Kilpatrick, Diana C. Alcobia, Carl W. White, Chloe J. Peach, Jackie R. Glenn, Kris Zimmerman, Alexander Kondrashov, Kevin D.G. Pfleger, Rachel Friedman Ohana, Matthew B. Robers, Keith V. Wood, Erica K. Sloan, Jeanette Woolard, Stephen J. Hill
Cell Chemical Biology, 2019
A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A3 receptor
Monica Bouzo-Lorenzo, Leigh A. Stoddart, Lizi Xia, Adriaan P. IJzerman, Laura H. Heitman, Stephen J. Briddon, Stephen J. Hill
Purinergic Signalling, 2019
Binding kinetics of ligands acting at GPCRs
David A. Sykes, Leigh A. Stoddart, Laura E. Kilpatrick, Stephen J. Hill
Molecular and Cellular Endocrinology, 2019
Probe dependence of allosteric enhancers on the binding affinity of adenosine A 1 -receptor agonists at rat and human A 1 -receptors measured using NanoBRET
Samantha L. Cooper, Mark Soave, Manuela Jörg, Peter J. Scammells, Jeanette Woolard, Stephen J. Hill
British Journal of Pharmacology, 2019
A non-functional galanin receptor-2 in a multiple sclerosis patient
Sheila Garcia-Rosa, Daniela BB Trivella, Vanessa D Marques, Rodolfo B Serafim, José GC Pereira, Julio CC Lorenzi, Greice A Molfetta, Paulo P Christo, Guilherme S Olival, Vania BT Marchitto, Doralina G Brum, Thais S Sabedot, Houtan Noushmehr, Alessandro S Farias, Leonilda MB Santos, José A Nogueira-Machado, Jorge ES Souza, Camila M Romano, Rodrigo M Conde, Antonio C Santos, Carlos T Guerreiro, Willem H Schreuder, Frederico O Gleber-Netto, Maria Amorim, Renan Valieris, Israel Tojal da Silva, Wilson A Silva, Diana N Nunes, Paulo SL Oliveira, Valeria Valente, Maria Augusta Arruda, Stephen J Hill, Amilton A Barreira, Emmanuel Dias-Neto
Pharmacogenomics Journal, 2019
Structure-based exploration and pharmacological evaluation of N-substituted piperidin-4-yl-methanamine CXCR4 chemokine receptor antagonists
I. Adlere, S. Sun, A. Zarca, L. Roumen, M. Gozelle, C. Perpiñá Viciano, B. Caspar, M. Arimont, J.P. Bebelman, S.J. Briddon, C. Hoffmann, S.J. Hill, M.J. Smit, H.F. Vischer, M. Wijtmans, C. de Graaf, I.J.P. de Esch, R. Leurs
European Journal of Medicinal Chemistry, 2019
Comparison of the ligand-binding properties of fluorescent VEGF-A isoforms to VEGF receptor 2 in living cells and membrane preparations using NanoBRET
Chloe J. Peach, Laura E. Kilpatrick, Jeanette Woolard, Stephen J. Hill
British Journal of Pharmacology, 2019
Circulating epinephrine is not required for chronic stress to enhance metastasis
Adam K. Walker, Davide Martelli, Alexandra I. Ziegler, Gavin W. Lambert, Sarah E. Phillips, Stephen J. Hill, Robin M. McAllen, Erica K. Sloan
Psychoneuroendocrinology, 2019
Adenosine and Forskolin Inhibit Platelet Aggregation by Collagen but not the Proximal Signalling Events
Joanne C. Clark, Deirdre M. Kavanagh, Stephanie Watson, Jeremy A. Pike, Robert K. Andrews, Elizabeth E. Gardiner, Natalie S. Poulter, Stephen J. Hill, Steve P. Watson
Thrombosis and Haemostasis, 2019
Development of novel fluorescent histamine H1-receptor antagonists to study ligand-binding kinetics in living cells
Leigh A. Stoddart, Andrea J. Vernall, Monica Bouzo-Lorenzo, Reggie Bosma, Albert J. Kooistra, Chris de Graaf, Henry F. Vischer, Rob Leurs, Stephen J. Briddon, Barrie Kellam, Stephen J. Hill
Scientific Reports, 2018
Real-Time Ligand Binding of Fluorescent VEGF-A Isoforms that Discriminate between VEGFR2 and NRP1 in Living Cells
Chloe J. Peach, Laura E. Kilpatrick, Rachel Friedman-Ohana, Kris Zimmerman, Matthew B. Robers, Keith V. Wood, Jeanette Woolard, Stephen J. Hill
Cell Chemical Biology, 2018
Visualizing Ligand Binding to a GPCR In Vivo Using NanoBRET
Diana C. Alcobia, Alexandra I. Ziegler, Alexander Kondrashov, Eleonora Comeo, Sarah Mistry, Barrie Kellam, Aeson Chang, Jeanette Woolard, Stephen J. Hill, Erica K. Sloan
Iscience, 2018
Molecular pharmacology of VEGF-A isoforms: Binding and signalling at VEGFR2
Chloe J. Peach, Viviane W. Mignone, Maria Augusta Arruda, Diana C. Alcobia, Stephen J. Hill, Laura E. Kilpatrick, Jeanette Woolard
International Journal of Molecular Sciences, 2018
Synthesis and Evaluation of the First Fluorescent Antagonists of the Human P2Y 2 Receptor Based on AR-C118925
Sean Conroy, Nicholas D. Kindon, Jacqueline Glenn, Leigh A. Stoddart, Richard J. Lewis, Stephen J. Hill, Barrie Kellam, Michael J. Stocks
Journal of Medicinal Chemistry, 2018
Fluorescence Approaches Unravel Spatial and Temporal Aspects of GPCR Organisation, Location, and Intracellular Signalling
Stephen J. Hill, Stephen P. Watson
Trends in Pharmacological Sciences, 2018
NanoBRET Approaches to Study Ligand Binding to GPCRs and RTKs
Leigh A. Stoddart, Laura E. Kilpatrick, Stephen J. Hill
Trends in Pharmacological Sciences, 2018
Studying GPCR Pharmacology in Membrane Microdomains: Fluorescence Correlation Spectroscopy Comes of Age
Stephen J. Briddon, Laura E. Kilpatrick, Stephen J. Hill
Trends in Pharmacological Sciences, 2018
Characterisation of endogenous A2A and A2B receptor-mediated cyclic AMP responses in HEK 293 cells using the GloSensor™ biosensor: Evidence for an allosteric mechanism of action for the A2B-selective antagonist PSB 603
Joelle Goulding, Lauren T. May, Stephen J. Hill
Biochemical Pharmacology, 2018
A monoclonal antibody raised against a thermo-stabilised β1-adrenoceptor interacts with extracellular loop 2 and acts as a negative allosteric modulator of a sub-set of β1-adrenoceptors expressed in stable cell lines
Mark Soave, Gabriella Cseke, Catherine J. Hutchings, Alastair J.H. Brown, Jeanette Woolard, Stephen J. Hill
Biochemical Pharmacology, 2018
Synthesis of novel (benzimidazolyl)isoquinolinols and evaluation as adenosine A1 receptor tools
Sameek Singh, Samantha L. Cooper, Jacqueline R. Glenn, Jessica Beresford, Lydia R. Percival, Joel D. A. Tyndall, Stephen J. Hill, Laura E. Kilpatrick, Andrea J. Vernall
Rsc Advances, 2018
A non-imaging high throughput approach to chemical library screening at the unmodified adenosine-A3 receptor in living cells
Maria Augusta Arruda, Leigh A. Stoddart, Karolina Gherbi, Stephen J. Briddon, Barrie Kellam, Stephen J. Hill
Frontiers in Pharmacology, 2017
Real-time analysis of the binding of fluorescent VEGF165a to VEGFR2 in living cells: Effect of receptor tyrosine kinase inhibitors and fate of internalized agonist-receptor complexes
Laura E. Kilpatrick, Rachel Friedman-Ohana, Diana C. Alcobia, Kristin Riching, Chloe J. Peach, Amanda J. Wheal, Stephen J. Briddon, Matthew B. Robers, Kris Zimmerman, Thomas Machleidt, Keith V. Wood, Jeanette Woolard, Stephen J. Hill
Biochemical Pharmacology, 2017
Novel selective β1-adrenoceptor antagonists for concomitant cardiovascular and respiratory disease
Jillian G. Baker, Sheila M. Gardiner, Jeanette Woolard, Christophe Fromont, Gopal P. Jadhav, Shailesh N. Mistry, Kevin S. J. Thompson, Barrie Kellam, Stephen J. Hill, Peter M. Fischer
FASEB Journal, 2017
Design and Elaboration of a Tractable Tricyclic Scaffold To Synthesize Druglike Inhibitors of Dipeptidyl Peptidase-4 (DPP-4), Antagonists of the C-C Chemokine Receptor Type 5 (CCR5), and Highly Potent and Selective Phosphoinositol-3 Kinase δ (PI3Kδ) Inhibitors
Carolin Schwehm, Barrie Kellam, Aimie E. Garces, Stephen J. Hill, Nicholas D. Kindon, Tracey D. Bradshaw, Jin Li, Simon J. F. Macdonald, James E. Rowedder, Leigh A. Stoddart, Michael J. Stocks
Journal of Medicinal Chemistry, 2017
Structure-activity relationships of the sustained effects of adenosine A2A receptor agonists driven by slow dissociation kinetics
J. Daniel Hothersall, Dong Guo, Sunil Sarda, Robert J. Sheppard, Hongming Chen, Wesley Keur, Michael J. Waring, Adriaan P. IJzerman, Stephen J. Hill, Ian L. Dale, Philip B. Rawlins
Molecular Pharmacology, 2017
Use of a new proximity assay (NanoBRET) to investigate the ligand-binding characteristics of three fluorescent ligands to the human β1-adrenoceptor expressed in HEK-293 cells
Mark Soave, Leigh A. Stoddart, Alastair Brown, Jeanette Woolard, Stephen J. Hill
Pharmacology Research and Perspectives, 2016
The use of fluorescence correlation spectroscopy to characterize the molecular mobility of fluorescently labelled G protein-coupled receptors
Laura E. Kilpatrick, Stephen J. Hill
Biochemical Society Transactions, 2016
Fluorescence- and bioluminescence-based approaches to study GPCR ligand binding
Leigh A Stoddart, Carl W White, Kim Nguyen, Stephen J Hill, Kevin D G Pfleger
British Journal of Pharmacology, 2016
Fragment-Based Discovery of Subtype-Selective Adenosine Receptor Ligands from Homology Models
Anirudh Ranganathan, Leigh A. Stoddart, Stephen J. Hill, Jens Carlsson
Journal of Medicinal Chemistry, 2015
Investigation of GPCR allosterism and dimerization in single living cells using fluorescent ligands
Stehen Hill
Springerplus, 2015
Probing the pharmacology of G protein-coupled receptors with fluorescent ligands
Leigh A. Stoddart, Laura E. Kilpatrick, Stephen J. Briddon, Stephen J. Hill
Neuropharmacology, 2015
Direct visualisation of internalization of the adenosine A3 receptor and localization with arrestin3 using a fluorescent agonist
Leigh A. Stoddart, Andrea J. Vernall, Stephen J. Briddon, Barrie Kellam, Stephen J. Hill
Neuropharmacology, 2015
Ligand residence time at G-protein-coupled receptors - Why we should take our time to study it
C. Hoffmann, M. Castro, A. Rinken, R. Leurs, S.J. Hill, H.F. Vischer
Molecular Pharmacology, 2015
A perspective on studying G-protein-coupled receptor signaling with resonance energy transfer biosensors in living organisms
Jakobus van Unen, Jeanette Woolard, Ago Rinken, Carsten Hoffmann, Stephen J. Hill, Joachim Goedhart, Michael R. Bruchas, Michel Bouvier, Merel J.W. Adjobo-Hermans
Molecular Pharmacology, 2015
Negative cooperativity across β1-adrenoceptor homodimers provides insights into the nature of the secondary low-affinity CGP 12177 β1-adrenoceptor binding conformation
Karolina Gherbi, Lauren T. May, Jillian G. Baker, Stephen J. Briddon, Stephen J. Hill
FASEB Journal, 2015
Application of BRET to monitor ligand binding to GPCRs
Leigh A Stoddart, Elizabeth K M Johnstone, Amanda J Wheal, Joëlle Goulding, Matthew B Robers, Thomas Machleidt, Keith V Wood, Stephen J Hill, Kevin D G Pfleger
Nature Methods, 2015
Effects of receptor tyrosine kinase inhibitors on VEGF165a- and VEGF165b-stimulated gene transcription in HEK-293 cells expressing human VEGFR2
Joanne J Carter, Amanda J Wheal, Stephen J Hill, Jeanette Woolard
British Journal of Pharmacology, 2015
Histaminic Agonists and Antagonists
Stephen J. Hill
Encyclopedia of Psychopharmacology, 2015
Salmeterol's extreme β2 selectivity is due to residues in both extracellular loops and transmembrane domains
Jillian G. Baker, Richard G.W. Proudman, Stephen J. Hill
Molecular Pharmacology, 2015
Detection of the secondary, low-affinity β1-adrenoceptor site in living cells using the fluorescent CGP 12177 derivative BODIPY-TMR-CGP
K Gherbi, S J Briddon, S J Hill
British Journal of Pharmacology, 2014
Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism
Ross Corriden, Laura E. Kilpatrick, Barrie Kellam, Stephen J. Briddon, Stephen J. Hill
FASEB Journal, 2014
The evolving small-molecule fluorescent-conjugate toolbox for Class A GPCRs
Andrea J Vernall, Stephen J Hill, Barrie Kellam
British Journal of Pharmacology, 2014
Identification of key residues in transmembrane 4 responsible for the secondary, low-affinity conformation of the human β1-adrenoceptor
Jillian G. Baker, Richard G.W. Proudman, Stephen J. Hill
Molecular Pharmacology, 2014
Biophysical detection of diversity and bias in GPCR function
Werner C. Jaeger, Stephen P. Armstrong, Stephen J. Hill, Kevin D. G. Pfleger
Frontiers in Endocrinology, 2014
Effect of a toggle switch mutation in TM6 of the human adenosine A 3 receptor on Gi protein-dependent signalling and Gi-independent receptor internalization
Leigh A Stoddart, Barrie Kellam, Stephen J Briddon, Stephen J Hill
British Journal of Pharmacology, 2014
Allosteric interactions at adenosine A1 and A3 receptors: New insights into the role of small molecules and receptor dimerization
Stephen J Hill, Lauren T May, Barrie Kellam, Jeanette Woolard
British Journal of Pharmacology, 2014
Monoclonal anti-β1-adrenergic receptor antibodies activate G protein signaling in the absence of β-arrestin recruitment
Catherine J Hutchings, Gabriella Cseke, Greg Osborne, Jeanette Woolard, Andrei Zhukov, Markus Koglin, Ali Jazayeri, Jahnavi Pandya-Pathak, Christopher J Langmead, Stephen J Hill, Malcolm Weir, Fiona H. Marshall
Mabs, 2014
Impact of polymorphic variants on the molecular pharmacology of the two-agonist conformations of the human β1-adrenoceptor
Jillian G. Baker, Richard G. W. Proudman, Stephen J. Hill
Plos One, 2013
Conversion of a non-selective adenosine receptor antagonist into A 3-selective high affinity fluorescent probes using peptide-based linkers
Andrea J. Vernall, Leigh A. Stoddart, Stephen J. Briddon, Hui Wen Ng, Charles A. Laughton, Stephen W. Doughty, Stephen J. Hill, Barrie Kellam
Organic and Biomolecular Chemistry, 2013
Fluorescent ligands for G protein-coupled receptors: Illuminating receptor-ligand interactions for drug discovery
Leigh A Stoddart, Stephen J Briddon, Stephen J Hill
Future Medicinal Chemistry, 2013
Adenosine-A 3 receptors in neutrophil microdomains promote the formation of bacteria-tethering cytonemes
Ross Corriden, Tim Self, Kathryn Akong‐Moore, Victor Nizet, Barrie Kellam, Stephen J Briddon, Stephen J Hill
EMBO Reports, 2013
Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists
Shailesh N. Mistry, Jillian G Baker, Peter M Fischer, Stephen J Hill, Sheila M Gardiner, Barrie Kellam
Journal of Medicinal Chemistry, 2013
Fragment screening at adenosine-A3 receptors in living cells using a fluorescence-based binding assay
Leigh A. Stoddart, Andrea J. Vernall, Jessica L. Denman, Stephen J. Briddon, Barrie Kellam, Stephen J. Hill
Chemistry and Biology, 2012
A novel fluorescent histamine H 1 receptor antagonist demonstrates the advantage of using fluorescence correlation spectroscopy to study the binding of lipophilic ligands
Rachel H Rose, Stephen J Briddon, Stephen J Hill
British Journal of Pharmacology, 2012
New potent, short-linker BODIPY-630/650™ labelled fluorescent adenosine receptor agonists
Clare L. Dale, Stephen J. Hill, Barrie Kellam
Medchemcomm, 2012
Highly potent and selective fluorescent antagonists of the human adenosine A3 receptor based on the 1,2,4-triazolo[4,3-a]quinoxalin-1-one scaffold
Andrea J. Vernall, Leigh A. Stoddart, Stephen J. Briddon, Stephen J. Hill, Barrie Kellam
Journal of Medicinal Chemistry, 2012
Adenylyl cyclase AC8 directly controls its micro-environment by recruiting the actin cytoskeleton in a cholesterol-rich milieu
Laura J. Ayling, Stephen J. Briddon, Michelle L. Halls, Gerald R. V. Hammond, Luis Vaca, Jonathan Pacheco, Stephen J. Hill, Dermot M. F. Cooper
Journal of Cell Science, 2012
Predicting in vivo cardiovascular properties of β-blockers from cellular assays: A quantitative comparison of cellular and cardiovascular pharmacological responses
Jillian G. Baker, Philip Kemp, Julie March, Laurice Fretwell, Stephen J. Hill, Sheila M. Gardiner
FASEB Journal, 2011
Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a- diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors
Jillian G. Baker, Luke A. Adams, Karolina Salchow, Shailesh N. Mistry, Richard J. Middleton, Stephen J. Hill, Barrie Kellam
Journal of Medicinal Chemistry, 2011
Allosteric interactions across native adenosine-A 3 receptor homodimers: Quantification using single-cell ligand-binding kinetics
Lauren T. May, Lloyd J. Bridge, Leigh A. Stoddart, Stephen J. Briddon, Stephen J. Hill
FASEB Journal, 2011
Evolution of β-blockers: From anti-anginal drugs to ligand-directed signalling
Jillian G. Baker, Stephen J. Hill, Roger J. Summers
Trends in Pharmacological Sciences, 2011
Inhibition of tissue transglutaminase 2 attenuates contractility of pregnant human myometrium
J. Alcock, A. Y. Warren, Y. J. Goodson, S. J. Hill, R. N. Khan, J. S. Lymn
Biology of Reproduction, 2011
Design and use of fluorescent ligands to study ligand-receptor interactions in single living cells
Stephen J. Briddon, Barrie Kellam, Stephen J. Hill
Methods in Molecular Biology, 2011
Insights into GPCR pharmacology from the measurement of changes in intracellular cyclic AMP; advantages and pitfalls of differing methodologies
Stephen J Hill, Christine Williams, Lauren T May
British Journal of Pharmacology, 2010
Modelling of the activation of G-protein coupled receptors: Drug free constitutive receptor activity
P. J. Woodroffe, L. J. Bridge, J. R. King, C. Y. Chen, S. J. Hill
Journal of Mathematical Biology, 2010
The Evolving Pharmacology of GPCRs
Lauren T. May, Nicholas D. Holliday, Stephen J. Hill
Gpcr Molecular Pharmacology and Drug Targeting Shifting Paradigms and New Directions, 2010
Antagonist selective modulation of adenosine A1 and A 3 receptor pharmacology by the food dye brilliant black BN: Evidence for allosteric interactions
L.T. May, S.J. Briddon, S.J. Hill
Molecular Pharmacology, 2010
Mathematical modelling of signalling in a two-ligand G-protein coupled receptor system: Agonist-antagonist competition
L.J. Bridge, J.R. King, S.J. Hill, M.R. Owen
Mathematical Biosciences, 2010
Influence of fluorophore and linker composition on the pharmacology of fluorescent adenosine A 1 receptor ligands: Themed section: Imaging in pharmacology research paper
Jillian G Baker, Richard Middleton, Luke Adams, Lauren T May, Stephen J Briddon, Barrie Kellam, Stephen J Hill
British Journal of Pharmacology, 2010
Use of Fluorescence Correlation Spectroscopy to Study the Diffusion of G Protein-coupled Receptors
Stephen J. Briddon, Jonathan A. Hern, Stephen J. Hill
G Protein Coupled Receptors Essential Methods, 2010
Quantitative analysis of neuropeptide y receptor association with β-arrestin2 measured by bimolecular fluorescence complementation
LE Kilpatrick, SJ Briddon, SJ Hill, ND Holliday
British Journal of Pharmacology, 2010
The effect of allosteric modulators on the kinetics of agonist-G protein-coupled receptor interactions in single living cells
Lauren T. May, Tim J. Self, Stephen J. Briddon, Stephen J. Hill
Molecular Pharmacology, 2010
Modelling the activation of G-protein coupled receptors by a single drug
P.J. Woodroffe, L.J. Bridge, J.R. King, S.J. Hill
Mathematical Biosciences, 2009
GPCR signaling: understanding the pathway to successful drug discovery.
Christine Williams, Stephen J. Hill
Methods in Molecular Biology Clifton N J, 2009
Role of key transmembrane residues in agonist and antagonist actions at the two conformations of the human β1-adrenoceptor
Jillian G. Baker, Richard G.W. Proudman, Nicola C. Hawley, Peter M. Fischer, Stephen J. Hill
Molecular Pharmacology, 2008
Quantitative profiling of nucleotides and related phosphate-containing metabolites in cultured mammalian cells by liquid chromatography tandem electrospray mass spectrometry
Rebecca L. Cordell, Stephen J. Hill, Catharine A. Ortori, David A. Barrett
Journal of Chromatography B Analytical Technologies in the Biomedical and Life Sciences, 2008
ERK phosphorylation: Spatial and temporal regulation by G protein-coupled receptors
Lauren T. May, Stephen J. Hill
International Journal of Biochemistry and Cell Biology, 2008
Effect of CCR5 receptor antagonists on endocytosis of the human CCR5 receptor in CHO-K1 cells
J Longden, E‐L Cooke, S J Hill
British Journal of Pharmacology, 2008
Agonist-occupied A3 adenosine receptors exist within heterogeneous complexes in membrane microdomains of individual living cells
Y. Cordeaux, S. J. Briddon, S. P. H. Alexander, B. Kellam, S. J. Hill
FASEB Journal, 2008
Plasma membrane diffusion of g protein-coupled receptor oligomers
Stephen J. Briddon, Jorge Gandía, Olavo B. Amaral, Sergi Ferré, Carme Lluís, Rafael Franco, Stephen J. Hill, Francisco Ciruela
Biochimica Et Biophysica Acta Molecular Cell Research, 2008
Pharmacology under the microscope: the use of fluorescence correlation spectroscopy to determine the properties of ligand-receptor complexes
Stephen J. Briddon, Stephen J. Hill
Trends in Pharmacological Sciences, 2007
Multiple GPCR conformations and signalling pathways: implications for antagonist affinity estimates
Jillian G. Baker, Stephen J. Hill
Trends in Pharmacological Sciences, 2007
New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains of single living cells
Richard J. Middleton, Stephen J. Briddon, Yolande Cordeaux, Andrew S. Yates, Clare L. Dale, Michael W. George, Jillian. G. Baker, Stephen J. Hill, Barrie Kellam
Journal of Medicinal Chemistry, 2007
A Comparison of the antagonist affinities for the Gi- and G s-coupled states of the human adenosine A1-receptor
Jillian G. Baker, Stephen J. Hill
Journal of Pharmacology and Experimental Therapeutics, 2007
Transgenic enrichment of cardiomyocytes from human embryonic stem cells
David Anderson, Tim Self, Ian R Mellor, Gareth Goh, Stephen J Hill, Chris Denning
Molecular Therapy, 2007
G-protein-coupled receptors: Past, present and future
Stephen J Hill
British Journal of Pharmacology, 2006
Characterization of isoprenaline- and salmeterol-stimulated interactions between β2-adrenoceptors and β-arrestin 2 using β-galactosidase complementation in C2C12 cells
Alison A. Carter, Stephen J. Hill
Journal of Pharmacology and Experimental Therapeutics, 2005
Clathrin-independent internalization of the human histamine H 1-receptor in CHO-K1 cells
Timothy J Self, Sarah M Oakley, Stephen J Hill
British Journal of Pharmacology, 2005
Trypsin stimulates the phosphorylation of p42,44 mitogen-activated protein kinases via the proteinase-activated receptor-2 and protein kinase C epsilon in human cultured prostate stromal cells
Andrew Myatt, Stephen J. Hill
Prostate, 2005
Oxytocin inhibits T-type calcium current of human decidual stromal cells
Bo Liu, Stephen J. Hill, Raheela N. Khan
Journal of Clinical Endocrinology and Metabolism, 2005
Coupling of the human A 1 adenosine receptor to different heterotrimeric G proteins: Evidence for agonist-specific G protein activation
Yolande Cordeaux, Adriaan P IJzerman, Stephen J Hill
British Journal of Pharmacology, 2004
Temporal Characteristics of cAMP Response Element-Mediated Gene Transcription: Requirement for Sustained cAMP Production
Jillian G Baker, Ian P Hall, Stephen J Hill
Molecular Pharmacology, 2004
Quantitative analysis of the formation and diffusion of A 1-adenosine receptor-antagonist complexes in single living cells
S. J. Briddon, R. J. Middleton, Y. Cordeaux, F. M. Flavin, J. A. Weinstein, M. W. George, B. Kellam, S. J. Hill
Proceedings of the National Academy of Sciences of the United States of America, 2004
Application of fluorescence correlation spectroscopy to the measurement of agonist binding to a G-protein coupled receptor at the single cell level
Stephen J. Briddon, Richard J. Middleton, Andrew S. Yates, Michael W. George, Barrie Kellam, Stephen J. Hill
Faraday Discussions, 2004
Agonist and Inverse Agonist Actions of β-Blockers at the Human β2-Adrenoceptor Provide Evidence for Agonist-Directed Signaling
Jillian G. Baker, Ian P. Hall, Stephen J. Hill
Molecular Pharmacology, 2003
Influence of agonist efficacy and receptor phosphorylation on antagonist affinity measurements: Differences between second messenger and reporter gene responses
Jillian G Baker, Ian P Hall, Stephen J Hill
Molecular Pharmacology, 2003
Agonist actions of "β-blockers" provide evidence for two agonist activation sites or conformations of the human β1-adrenoceptor
Jillian G. Baker, Ian P. Hall, Stephen J. Hill
Molecular Pharmacology, 2003
Comparison of potassium currents in human decidua before and after the onset of labor
Bo Liu, Sabaratnam Arulkumaran, Stephen J. Hill, Raheela N. Khan
Biology of Reproduction, 2003
Pharmacology and direct visualisation of BODIPY-TMR-CGP: A long-acting fluorescent β 2-adrenoceptor agonist
Jillian G Baker, Ian P Hall, Stephen J Hill
British Journal of Pharmacology, 2003
The ups and downs of Gs- to Gi-protein switching
Stephen J Hill, Jillian G Baker
British Journal of Pharmacology, 2003
A role of protein kinase Cμ in signalling from the human adenosine A1 receptor to the nucleus
Kathryn J Hill, Anne C Webber, Stephen J Hill
British Journal of Pharmacology, 2003
Modelling of signalling via G-protein coupled receptors: Pathway-dependent agonist potency and efficacy
C Chen
Bulletin of Mathematical Biology, 2003
Mechanisms of cross-talk between G-protein-coupled receptors
Yolande Cordeaux, Stephen J. Hill
Neurosignals, 2002
The growth response of Escherichia coli to neurotransmitters and related catecholamine drugs requires a functional enterobactin biosynthesis and uptake system
Claire L. Burton, Siri Ram Chhabra, Simon Swift, Tom J. Baldwin, Helen Withers, Stephen J. Hill, Paul Williams
Infection and Immunity, 2002
Pharmacological characterization of CGP 12177 at the human β 2-adrenoceptor
Jillian G Baker, Ian P Hall, Stephen J Hill
British Journal of Pharmacology, 2002
Reporter-gene systems for the study of G-protein-coupled receptors
S Hill
Current Opinion in Pharmacology, 2001
Modulation by cellular cholesterol of gene transcription via the cyclic AMP response element
Aliya Middleton, David Nury, Susan J Willington, Liaque Latif, Stephen J Hill, Bruce Middleton
Biochemical Pharmacology, 2001
Role of protein kinase Cα in signaling from the histamine H1 receptor to the nucleus
A.C. Megson, E.M. Walker, S.J. Hill
Molecular Pharmacology, 2001
Non-competitive antagonism of β2-agonist-mediated cyclic AMP accumulation by ICI 118551 in BC3H1 cells endogenously expressing constitutively active β2-adrenoceptors
H E Hopkinson, M L Latif, S J Hill
British Journal of Pharmacology, 2000
Influence of receptor number on functional responses elicited by agonists acting at the human adenosine A1 receptor: Evidence for signaling pathway-dependent changes in agonist potency and relative intrinsic activity
Yolande Cordeaux, Stephen J. Briddon, Anne E. Megson, Jacqui McDonnell, John M. Dickenson, Stephen J. Hill
Molecular Pharmacology, 2000
Gi-protein α-subunit mRNA antisense oligonucleotide inhibition of Gi-coupled receptor contractile activity in the epididymis of the guinea-pig
John M Haynes, Lisa A Selbie, Stephen J Hill
British Journal of Pharmacology, 1999
Nonselective effects of the putative phospholipase C inhibitor, U73122, on adenosine A1 receptor-mediated signal transduction events in Chinese hamster ovary cells
Elizabeth M. Walker, Jayson R. Bispham, Stephen J. Hill
Biochemical Pharmacology, 1998
Potentiation of adenosine A1 receptor-mediated inositol phospholipid hydrolysis by tyrosine kinase inhibitors in CHO cells
John M. Dickenson, Stephen J. Hill
British Journal of Pharmacology, 1998
Influence of receptor number on the stimulation by salmeterol of gene transcription in CHO-K1 cells transfected with the human β2-adrenoceptor
J McDonnell, M L Latif, E S Rees, N J Bevan, S J Hill
British Journal of Pharmacology, 1998
A1 and A2 adenosine receptor modulation of contractility in the cauda epididymis of the guinea-pig
John M Haynes, S P H Alexander, Stephen J Hill
British Journal of Pharmacology, 1998
Human adenosine A1 receptor and P2Y2-purinoceptor-mediated activation of the mitogen-activated protein kinase cascade in transfected CHO cells
John M. Dickenson, Jonathan L. Blank, Stephen J. Hill
British Journal of Pharmacology, 1998
Involvement of G-protein βγ subunits in coupling the adenosine A1 receptor to phospholipase C in transfected CHO cells
John M. Dickenson, Stephen J. Hill
European Journal of Pharmacology, 1998
A1 adenosine receptor modulation of electrically-evoked contractions in the bisected vas deferens and cauda epididymis of the guinea-pig
John M. Haynes, S P H. Alexander, Stephen J. Hill
British Journal of Pharmacology, 1998
Human 5-HT(1B) receptor stimulated inositol phospholipid hydrolysis in CHO cells: Synergy with G(q)-coupled receptors
John M Dickenson, Stephen J Hill
European Journal of Pharmacology, 1998
G protein-coupled-receptor cross-talk: The fine-tuning of multiple receptor-signalling pathways
L.A. Selbie, S.J. Hill
Trends in Pharmacological Sciences, 1998
Receptor-stimulated phospholipase C activity in human umbilical artery cultured endothelial cells grown in a low oxygen environment
K.A. Marsh, L.M. Draper, P.C. Rubin, S.J. Hill
Biochemical Pharmacology, 1997
β-Adrenoceptor-mediated inhibition of α1-adrenoceptor-mediated and field stimulation-induced contractile responses in the prostate of the guinea pig
John M. Haynes, Stephen J. Hill
British Journal of Pharmacology, 1997
Detrusor instability - Is it due to defective receptor desensitization?
British Journal of Urology, 1997
Role of G-protein βγ subunits in the augmentation of P2Y2 (P2U) receptor-stimulated responses by neuropeptide Y Y1 Gi/o-coupled receptors
A. Lisa SELBIE, V. Natalie KING, M. John DICKENSON, J. Stephen HILL
Biochemical Journal, 1997
An endogenous A(2B) adenosine receptor coupled to cyclic AMP generation in human embryonic kidney (HEK 293) cells
Jacqui Cooper, Stephen J. Hill, Stephen P. H. Alexander
British Journal of Pharmacology, 1997
Transfected adenosine A1 receptor-mediated modulation of thrombin-stimulated phospholipase C and phospholipase A2 activity in CHO cells
John M. Dickenson, Stephen J. Hill
European Journal of Pharmacology, 1997
Neuropeptide Y (NPY) and peptide YY (PYY) effects in the epididymis of the guinea-pig: Evidence of a pre-junctional PYY-selective receptor
John M. Haynes, Stephen J. Hill, Lisa A. Selbie
British Journal of Pharmacology, 1997
International union of pharmacology. XIII. Classification of histamine receptors
S.J. Hill, C.R. Ganellin, H. Timmerman, J.C. Schwartz, N.P. Shankley, J.M. Young, W. Schunack, R. Levi, H.L. Haas
Pharmacological Reviews, 1997
Adenosine A1 receptor-mediated inhibition of cyclic AMP accumulation in type-2 but not type-1 rat astrocytes
Marie-Claire Peakman, Stephen J. Hill
European Journal of Pharmacology, 1996
Comparison of duration of agonist action at β1- and β2-adrenoceptors in C6 glioma cells: Evidence that the long duration of action of salmeterol Is specific to the β2-adrenoceptor
Molecular Pharmacology, 1996
Synergistic interactions between human transfected adenosine A1 receptors and endogenous cholecystokinin receptors in CHO cells
John M. Dickenson, Stephen J. Hill
European Journal of Pharmacology, 1996
Sensitivity of histamine H3 receptor agonist-stimulated [35S]GTPγ[S] binding to pertussis toxin
Elizabeth A. Clark, Stephen J. Hill
European Journal of Pharmacology, 1996
α-Adrenoceptor mediated responses of the cauda epididymis of the guinea-pig
John M. Haynes, Stephen J. Hill
British Journal of Pharmacology, 1996
Desensitization of muscarinic receptor-coupled inositol phospholipid hydrolysis in human detrusor cultured smooth muscle cells
K.A. Marsh, D.R. Harriss, S.J. Hill
Journal of Urology, 1996
Characterization of the human brain putative A(2B) adenosine receptor expressed in Chinese hamster ovary (CHO.A(2B4)) cells
Stephen P.H. Alexander, Jacqui Cooper, John Shine, Stephen J. Hill
British Journal of Pharmacology, 1996
Distribution of receptors mediating phosphoinositide hydrolysis in cultured human umbilical artery smooth muscle and endothelial cells
J. Hawley, P.C. Rubin, S.J. Hill
Biochemical Pharmacology, 1995
Activation of phospholipase C by G-protein βγ subunits in DDT1MF-2 cells
John M. Dickenson, Montserrat Camps, Peter Gierschik, Stephen J. Hill
European Journal of Pharmacology Molecular Pharmacology, 1995
Activation of Phospholipase C by G-protein βγ subunits in DDT1MF-2 cells
JOHN M. DICKENSON, STEPHEN J. HILL
Biochemical Society Transactions, 1995
Coupling of an endogenous 5‐HT1B‐like receptor to increases in intracellular calcium through a pertussis toxin‐sensitive mechanism in CHO‐K1 cells
John M. Dickenson, Stephen J. Hill
British Journal of Pharmacology, 1995
Adenosine A1 receptor‐mediated changes in basal and histamine‐stimulated levels of intracellular calcium in primary rat astrocytes
Marie‐Claire Peakman, Stephen J. Hill
British Journal of Pharmacology, 1995
Differential effect of sodium ions and guanine nucleotides on the binding of thioperamide and clobenpropit to histamine H3‐receptors in rat cerebral cortical membranes
E.A. Clark, S.J. Hill
British Journal of Pharmacology, 1995
Synergy between the inositol phosphate responses to transfected human adenosine A1‐receptors and constitutive P2‐purinoceptors in CHO‐K1 cells
Anne C. Megson, John M. Dickenson, Andrea Townsend‐Nicholson, Stephen J Hill
British Journal of Pharmacology, 1995
Expression of Muscarinic M sub 3 -Receptors Coupled to Inositol Phospholipid Hydrolysis in Human Detrusor Cultured Smooth Muscle Cells
D.R. Harriss, K.A. Marsh, A.T. Birmingham, S.J. Hill
Journal of Urology, 1995
Adenosine receptor‐induced cyclic AMP generation and inhibition of 5‐ hydroxytryptamine release in human platelets.
JA Cooper, SJ Hill, SP Alexander, PC Rubin, EH Horn
British Journal of Clinical Pharmacology, 1995
Selective potentiation of histamine H1-receptor stimulated calcium responses by 1,4-dithiothreitol in DDT1MF-2 cells
John M. Dickenson, Stephen J. Hill
Biochemical Pharmacology, 1994
Characteristics of [3H]mepyramine binding in DDT1MF-2 cells: Evidence for high affinity binding to a functional histamine H1 receptor
John M. Dickenson, Stephen J. Hill
European Journal of Pharmacology Molecular Pharmacology, 1994
Bradykinin B2- and 5-hydroxytryptamine (5-HT2)-receptor stimulated increases in intracellular calcium in cultured guinea-pig aortic smooth muscle cells
John M. Dickenson, Susan Bulmer, Andrea Whittaker, Michael Salwey, Julie Hawley, Stephen J. Hill
Biochemical Pharmacology, 1994
Des‐Arg9‐bradykinin‐induced increases in intracellular calcium ion concentration in single bovine tracheal smooth muscle cells
Katrina A. Marsh, Stephen J. Hill
British Journal of Pharmacology, 1994
Interactions between adenosine A1- and histamine H1-receptors
John M. Dickenson, Stephen J. Hill
International Journal of Biochemistry, 1994
Adenosine A2B‐receptor‐mediated cyclic AMP accumulation in primary rat astrocytes
Marie‐Claire Peakman, Stephen J. Hill
British Journal of Pharmacology, 1994
Endogenous expression of histamine H1 receptors functionally coupled to phosphoinositide hydrolysis in C6 glioma cells: regulation by cyclic AMP
Marie‐Claire Peakman, Stephen J. Hill
British Journal of Pharmacology, 1994
Coupling of a transfected human brain A1 adenosine receptor in CHO‐K1 cells to calcium mobilisation via a pertussis toxin‐sensitive mechanism
Philip A. Iredale, Stephen P.H. Alexander, Stephen J. Hill
British Journal of Pharmacology, 1994
Agonist‐induced desensitization of histamine Hi receptor‐mediated inositol phospholipid hydrolysis in human umbilical vein endothelial cells
G. McCreath, LP. Hall, S.J. Hill
British Journal of Pharmacology, 1994
A1 adenosine receptor inhibition of cyclic AMP formation and radioligand binding in the guinea‐pig cerebral cortex
Stephen P.H. Alexander, Alistair R. Curtis, David A. Kendall, Stephen J. Hill
British Journal of Pharmacology, 1994
A comparison of A2 adenosine receptor‐induced cyclic AMP generation in cerebral cortex and relaxation of pre‐contracted aorta
Stephen P.H. Alexander, Amanda Losinski, David A. Kendall, Stephen J. Hill
British Journal of Pharmacology, 1994
High, stable expression of the bovine histamine h1-receptor coupled to [Ca2+]i mobilization in CHO-K1 cells
P.A. Iredale, H. Fukui, S.J. Hill
Biochemical and Biophysical Research Communications, 1993
The effects of β-phorbol-12,13 dibutyrate on agonist-induced increases in [Ca2+]i in N1E-115 cells. Differential modulation of responses to angiotensin II and bradykinin
Philip A. Iredale, Keith F. Martin, Stephen J. Hill, David A. Kendall
Biochemical Pharmacology, 1993
The control of intracellular calcium and neurotransmitter release in guinea pig-derived cerebral cortical synaptoneurosomes
Philip A. Iredale, Keith F. Martin, Stephen J. Hill, David A. Kendall
Biochemical Pharmacology, 1993
Coupling of histamine H1 and Adenosine A1 receptors to phospholipase C in DDT1MF-2 cells: Synergistic interactions and regulation by cyclic AMP
John M. Dickenson, Stephen J. Hill
Biochemical Society Transactions, 1993
Salmeterol, a long‐acting β2‐adrenoceptor agonist mediating cyclic AMP accumulation in a neuronal cell line
Karen E. McCrea, Stephen J. Hill
British Journal of Pharmacology, 1993
Differential responses to histamine and cyclo-pentyladenosine in subclones of the DDT1MF-2 cell line
TERESA E. WHITE, STEPHEN J. HILL
Biochemical Society Transactions, 1993
Intracellular cross-talk between receptors coupled to phospholipase C via pertussis toxin sensitive and insensitive G-proteins
JOHN M. DICKENSON, STEPHEN J. HILL
Biochemical Society Transactions, 1993
Adenosine A1‐receptor stimulated increases in intracellular calcium in the smooth muscle cell line, DDT1MF‐2
John M. Dickenson, Stephen J. Hill
British Journal of Pharmacology, 1993
Intracellular cross‐talk between receptors coupled to phospholipase C via pertussis toxin‐sensitive and insensitive G‐proteins in DDT1MF‐2 cells
John M. Dickenson, Stephen J. Hill
British Journal of Pharmacology, 1993
Characteristics of the bradykinin‐induced changes in intracellular calcium ion concentration of single bovine tracheal smooth muscle cells
Katrina A. Marsh, Stephen J. Hill
British Journal of Pharmacology, 1993
Homologous and heterologous desensitization of histamine H1‐and ATP‐receptors in the smooth muscle cell line, DDT1MF‐2: the role of protein kinase C
John M. Dickenson, Stephen J. Hill
British Journal of Pharmacology, 1993
Increases in intracellular calcium via activation of an endogenous P2‐purinoceptor in cultured CHO‐K1 cells
Philip A. Iredale, Stephen J. Hill
British Journal of Pharmacology, 1993
Partial mediation by nitric oxide of the relaxation of human isolated detrusor strips in response to electrical field stimulation.
MJ James, AT Birmingham, SJ Hill
British Journal of Clinical Pharmacology, 1993
Histamine H1‐receptor‐mediated inositol phospholipid hydrolysis in DDT1MF‐2 cells: agonist and antagonist properties
Teresa E. White, John M. Dickenson, Stephen J. Hill
British Journal of Pharmacology, 1993
The effects of elevated cyclic AMP levels on histamine-H1-receptor-stimulated inositol phospholipid hydrolysis and calcium mobilization in the smooth-muscle cell line DDT1MF-2
J M Dickenson, T E White, S J Hill
Biochemical Journal, 1993
Significance of atropine concentration for the incidence of tetrodotoxin‐resistant relaxations of human detrusor strips
M. J. JAMES, D. R. HARRISS, A. T. BIRMINGHAM, S. J. HILL
British Journal of Clinical Pharmacology, 1993
Activation of a metabotropic excitatory amino acid receptor potentiates A2b adenosine receptor-stimulated cyclic AMP accumulation
Stephen P.H. Alexander, Alistair R. Curtis, Stephen J. Hill, David A. Kendall
Neuroscience Letters, 1992
Qualitative differences in [Ca2+]i increases and InsP3 generation following stimulation of N1E-115 cells with micromolar and millimolar ATP
Philip A. Iredale, Keith F. Martin, Stephen P.H. Alexander, Stephen J. Hill, David A. Kendall
Biochemical Pharmacology, 1992
Agonist-induced changes in [Ca2+]i in N1E-115 cells: differential effects of bradykinin and carbachol
Philip A. Iredale, Keith F. Martin, Stephen J. Hill, David A. Kendall
European Journal of Pharmacology Molecular Pharmacology, 1992
Effects of isozyme selective phosphodiesterase inhibitors on bovine tracheal smooth muscle tone
Ian P. Hall, Stephen J. Hill
Biochemical Pharmacology, 1992
Multiple histamine receptors: Properties and functional characteristics
Stephen J. Hill
Biochemical Society Transactions, 1992
Intracellular calcium measurements in response to histamine stimulation in DDT1, MF-2 cells
JOHN M. DICKENSON, STEPHEN J. HILL
Biochemical Society Transactions, 1992
Histamine H1-receptor-mediated calcium influx in DDT1MF-2 cells
J M Dickenson, S J Hill
Biochemical Journal, 1992
Bradykinin B2 receptor‐mediated phosphoinositide hydrolysis in bovine cultured tracheal smooth muscle cells
Katrina A. Marsh, Stephen J. Hill
British Journal of Pharmacology, 1992
Cross-talk between intracellular second messenger transduction systems
Drug News and Perspectives, 1992
Spermine enhances calcium- and GTP analogue-stimulated particulate phogphoinositidase
Biochemical Society Transactions, 1992
Excitatory Amino Acid‐Induced Phosphoinositide Turnover in Guinea Pig Cerebral Cortical Slices: Selective Enhancement by Spermine of the Response to DL‐1‐Aminocyclopentane‐ trans‐1, 3‐Dicarboxylate
Stephen P. H. Alexander, David A. Kendall, Stephen J. Hill
Journal of Neurochemistry, 1992
Expression of 5-HT2- and bradykinin B2-receptors coupled to phosphoinositide hydrolysis in cultured guinea-pig aortic smooth muscle cells
JULIE HAWLEY, PETER C. RUBIN, STEPHEN J. HILL
Biochemical Society Transactions, 1992
Adenosine A1‐receptor stimulation of inositol phospholipid hydrolysis and calcium mobilisation in DDT1 MF‐2 cells
Teresa E. White, John M. Dickenson, Stephen P.H. Alexander, Stephen J. Hill
British Journal of Pharmacology, 1992
Inositol 1,4,5‐trisphosphate generation and calcium mobilisation via activation of an atypical P2 receptor in the neuronal cell line, N1E‐115
Philip A. Iredale, Keith F. Martin, Stephen P.H. Alexander, Stephen J. Hill, David A. Kendall
British Journal of Pharmacology, 1992
Inhibition of Forskolin‐Stimulated Cyclic AMP Formation by 1‐Aminocyclopentane‐trans‐1,3‐Dicarboxylate in Guinea‐Pig Cerebral Cortical Slices
J. Cartmell, J. A. Kemp, S. P. H. Alexander, S. J. Hill, D. A. Kendall
Journal of Neurochemistry, 1992
Polyamine modulation of phosphoinositide responses to excitatory amino acids
Molecular Neuropharmacology, 1992
Do polyamines regulate the NMDA inhibition of muscarinic receptor-induced phosphoinositide turnover in guinea pig brain?
Stephen P.H. Alexander, Stephen J. Hill, David A. Kendall
Neuroscience Letters, 1991
Histamine-stimulated increases in intracellular calcium in the smooth muscle cell line, DDT1MF-2
John M. Dickenson, Stephen J. Hill
Biochemical Pharmacology, 1991
Adenosine receptor modulation of inositol phospholipid turnover in the central nervous system
Stephen Ph Alexander, Stephen J Hill, David A Kendall
Nucleosides and Nucleotides, 1991
α- and β-adrenoceptor regulation of cyclic AMP accumulation in cultured rat astrocytes. A comparison of primary protoplasmic and mixed fibrous/protoplasmic astroglial cultures
Angela Ruck, David A. Kendall, Stephen J. Hill
Biochemical Pharmacology, 1991
Histamine receptors and interactions between second messenger transduction systems
Stephen J. Hill
Agents and Actions, 1991
Histamine-induced changes in intracellular calcium in undifferentiated N1E-115 cells
PHILIP A. IREDALE, ANGELA RUCK, KEITH F. MARTIN, DAVID A. KENDALL, STEPHEN J. HILL
Biochemical Society Transactions, 1991
Expression of beta2-adrenoceptors mediating cyclic AMP accumulation in astroglial and neuronal cell lines derived from the rat CNS
Angela Ruck, Paul Millns, David A. Kendall, Stephen J. Hill
Biochemical Pharmacology, 1990
Differential effects of elevated calcium ion concentrations on inositol phospholipid responses in mouse and rat cerebral cortical slices
Stephen P.H. Alexander, Stephen J. Hill, David A. Kendall
Biochemical Pharmacology, 1990
Modulation of carbachol-induced inositol phosphate formation in bovine tracheal smooth muscle by cyclic AMP phosphodiesterase inhibitors
Ian P. Hall, Jill Donaldson, Stephen J. Hill
Biochemical Pharmacology, 1990
Distribution, properties, and functional characteristics of three classes of histamine receptor
Pharmacological Reviews, 1990
Discriminatory Effects of Forskolin and EGTA on the Indirect Cyclic AMP Responses to Histamine, Noradrenaline, 5‐Hydroxytryptamine, and Glutamate in Guinea‐Pig Cerebral Cortical Slices
J. Donaldson, D. A. Kendall, S. J. Hill
Journal of Neurochemistry, 1990
Agonist-induced contraction and accumulation of inositol phosphates in the guinea-pig detrusor: Evidence that muscarinic and purinergic receptors raise intracellular calcium by different mechanisms
J.W. Iacovou, S.J. Hill, A.T. Birmingham
Journal of Urology, 1990
Inositol phosphates accumulation in guinea pig cerebral cortical slices: Effects of protein kinase C activators and an inhibitor
S.P.H. Alexander, S.J. Hill, D.A. Kendall
European Journal of Pharmacology, 1990
Excitatory Amino Acid‐Induced Formation of Inositol Phosphates in Guinea‐Pig Cerebral Cortical Slices: Involvement of Ionotropic or Metabotropic Receptors?
Stephen P. H. Alexander, Stephen J. Hill, David A. Kendall
Journal of Neurochemistry, 1990
Characterization of histamine H3-receptors in guinea-pig ileum with H3-selective ligands
R.W.S. Hew, C.R. Hodgkinson, S.J. Hill
British Journal of Pharmacology, 1990
Modulation of fluoroaluminate-induced inositol phosphate formation by increases in tissue cyclic AMP content in bovine tracheal smooth muscle
I.P. Hall, J. Donaldson, S.J. Hill
British Journal of Pharmacology, 1990
Is the Adenosine Receptor Modulation of Histamine‐Induced Accumulation of Inositol Phosphates in Cerebral Cortical Slices Mediated by Effects on Calcium Ion Fluxes?
Stephen P. H. Alexander, Stephen J. Hill, David A. Kendall
Journal of Neurochemistry, 1990
Histamine receptors in brain vessels of guinea-pig: In-vitro pharmacology and ligand binding
A. OTTOSSON, S. J. HILL, L. EDVINSSON
Acta Physiologica Scandinavica, 1990
Effect of isozyme selective phosphodiesterase inhibitors on bovine tracheal smooth muscle tone
I.P. Hall, D. Walker, S.J. Hill, A.E. Tattersfield
European Journal of Pharmacology, 1990
Expression of β2-adrenoceptors mediating cyclic AMP accumulation in a neuronal cell line
S.J. Hill, A. Ruck, P. Millns, D.A. Kendall
European Journal of Pharmacology, 1990
Inhibition by salbutamol, forskolin and IBMX of AlF4-induced inositol phosphate formation in bovine airway smooth muscle.
British Journal of Pharmacology, 1989
The 2-chloroadenosine inhibition of histamine-induced inositol phosphates accumulation in mouse brain and calcium ions.
British Journal of Pharmacology, 1989
Cross-talk between different receptor-effector systems in the mammalian CNS
Stephen J. Hill, David A. Kendall
Cellular Signalling, 1989
Effect of Isozyme‐Selective Inhibitors of Phosphodiesterase on Histamine‐Stimulated Cyclic AMP Accumulation in Guinea‐Pig Hippocampus
Clare Stanley, Anthony M. Brown, Stephen J. Hill
Journal of Neurochemistry, 1989
Differences in the adenosine receptors modulating inositol phosphates and cyclic AMP accumulation in mammalian cerebral cortex
S.P.H. Alexander, D.A. Kendall, S.J. Hill
British Journal of Pharmacology, 1989
Inhibition of histamine-stimulated inositol phospholipid hydrolysis by agents which increase cyclic AMP levels in bovine tracheal smooth muscle
I.P. Hall, J. Donaldsona, S.J. Hill
British Journal of Pharmacology, 1989
Temporal changes in the calcium-dependence of the histamine H1-receptor-stimulation of cyclic AMP accumulation in guinea-pig cerebral cortex
Jill Donaldson, Anthony M. Brown, Stephen J. Hill
British Journal of Pharmacology, 1989
Calcium dependence and inositol phosphate accumulation in human detrusor smooth muscle
Neurourology and Urodynamics, 1989
Studies on the mechanism of histamine-induced release of noradrenaline and 5-hydroxytryptamine from slices of rat cerebral cortex
Catherine S. Young, Robert Mason, Stephen J. Hill
Biochemical Pharmacology, 1988
Inhibition by H1-antihistamines of the uptake of noradrenaline and 5-HT into rat brain synaptosomes
Catherine S. Young, Robert Mason, Stephen J. Hill
Biochemical Pharmacology, 1988
Influence of rolipram on the cyclic 3′,5′adenosine monophosphate response to histamine and adenosine in slices of guinea-pig cerebral cortex
Jill Donaldson, Anthony M. Brown, Stephen J. Hill
Biochemical Pharmacology, 1988
β ‐Adrenoceptor stimulation inhibits histamine‐stimulated inositol phospholipid hydrolysis in bovine tracheal smooth muscle
I.P. Hall, S.J. Hill
British Journal of Pharmacology, 1988
α 2‐Adrenoceptor‐mediated inhibition of histamine release from rat cerebral cortical slices
S.J. Hill, R.M. Straw
British Journal of Pharmacology, 1988
Adenosine Inhibition of Histamine‐Stimulated Inositol Phospholipid Hydrolysis in Mouse Cerebral Cortex
D. A. Kendall, S. J. Hill
Journal of Neurochemistry, 1988
Kinetic studies on the mechanism by which histamine H1 receptors potentiate cyclic AMP accumulation in guinea pig cerebral cortical slices
Molecular Pharmacology, 1988
Histamine Receptors in the Mammalian Central Nervous System: Biochemical Studies
S.J. Hill
Progress in Medicinal Chemistry, 1987
Histamine receptors branch out
Stephen J. Hill
Nature, 1987
1,4‐Dithiothreitol‐induced changes in histamine H1‐agonist efficacy and affinity in the longitudinal smooth muscle of guinea‐pig ileum
J. Donaldson, S.J. Hill
British Journal of Pharmacology, 1987
Studies on the adenosine‐receptor mediating the augmentation of histamine‐induced inositol phospholipid hydrolysis in guinea‐pig cerebral cortex
S.J. Hill, D.A. Kendall
British Journal of Pharmacology, 1987
The role of calcium in the cyclic AMP response to histamine in rabbit cerebral cortical slices
M. Al‐Gadi, S.J. Hill
British Journal of Pharmacology, 1987
1,4-dithiothreitol-induced alteration in histamine H1-agonist binding in guinea-pig cerebellum and cerebral cortex
Jill Donaldson, Stephen J. Hill
European Journal of Pharmacology, 1986
Histamine-induced hydrolysis of polyphosphoinositides in guinea-pig ileum and brain
Jill Donaldson, Stephen J. Hill
European Journal of Pharmacology, 1986
Selective enhancement of histamine H1‐receptor responses in guinea‐pig ileal smooth muscle by 1,4‐dithiothreitol
J. Donaldson, S.J. Hill
British Journal of Pharmacology, 1986
Enhancement of Histamine H1‐Receptor Agonist Activity by 1,4‐Dithiothreitol in Guinea‐Pig Cerebellum and Cerebral Cortex
J. Donaldson, S. J. Hill
Journal of Neurochemistry, 1986
Histamine‐induced inositol phospholipid breakdown in the longitudinal smooth muscle of guinea‐pig ileum
J. Donaldson, S.J. Hill
British Journal of Pharmacology, 1985
Characterization of histamine receptors mediating the stimulation of cyclic AMP accumulation in rabbit cerebral cortical slices
M. Al‐Gadi, S.J. Hill
British Journal of Pharmacology, 1985
The nature of the binding of [3H]mepyramine to homogenates of guinea-pig cerebral cortex at different [3H]ligand concentrations
Andrew J. Hadfield, Nicola R. Robinson, Stephen J. Hill
Biochemical Pharmacology, 1983
HISTAMINE H1‐AGONIST POTENTIATION OF ADENOSINE‐STIMULATED CYCLIC AMP ACCUMULATION IN SLICES OF GUINEA‐PIG CEREBRAL CORTEX: COMPARISON OF RESPONSE AND BINDING PARAMETERS
P.R. DAUM, S.J. HILL, J.M. YOUNG
British Journal of Pharmacology, 1982
Extended mepyramine treatment and histamine H1-receptors in guinea-pig brain
Stephen J. Hill, C. Robin Hiley, J. Michael Young
European Journal of Pharmacology, 1981
Characterization of [3H]mepyramine binding to the longitudinal muscle of guinea pig small intestine
Molecular Pharmacology, 1981
Histamine H1-receptors and cAMP accumulation in guinea-pig cerebral cortical slices
British Journal of Pharmacology, 1981
Affinities of Histamine H1‐Antagonists in Guinea Pig Brain: Similarity of Values Determined from [3H]Mepyramine Binding and from Inhibition of a Functional Response
S. J. Hill, P. Daum, J. M. Young
Journal of Neurochemistry, 1981
HISTAMINE H1‐RECEPTORS IN THE BRAIN OF THE GUINEA‐PIG AND THE RAT: DIFFERENCES IN LIGAND BINDING PROPERTIES AND REGIONAL DISTRIBUTION
S.J. HILL, J.M. YOUNG
British Journal of Pharmacology, 1980
The binding properties of [3H]-mepyramine in the brain of the guinea-pig and the rat
British Journal of Pharmacology, 1979
Antagonism of central histamine H1 receptors by antipsychotic drugs
Stephen J. Hill, Michael Young
European Journal of Pharmacology, 1978
Evidence for the presence of histamine H1-receptors in guinea-pig brain
British Journal of Pharmacology, 1978
THE BINDING OF [3H]MEPYRAMINE TO HISTAMINE H1 RECEPTORS IN GUINEA‐PIG BRAIN
S. J. Hill, P. C. Emson, J. M. Young
Journal of Neurochemistry, 1978
A convenient synthesis of [3H]mepyramine and certain related [3H]antihistamines
D H Marrian, S J Hill, J K M Sanders, J M Young
Journal of Pharmacy and Pharmacology, 1978
Specific binding of 3H-mepyramine to histamine H1 receptors in intestinal smooth muscle
S. J. HILL, J. M. YOUNG, D. H. MARRIAN
Nature, 1977

Stephen J Hill

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