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List of works by Stephen J. Hill

1,4-Dithiothreitol-induced alteration in histamine H1-agonist binding in guinea-pig cerebellum and cerebral cortex

scientific article

A Non-imaging High Throughput Approach to Chemical Library Screening at the Unmodified Adenosine-A3 Receptor in Living Cells

scientific article published on 13 December 2017

A Perspective on Studying G-Protein-Coupled Receptor Signaling with Resonance Energy Transfer Biosensors in Living Organisms

scientific article

A comparison of the antagonist affinities for the Gi- and Gs-coupled states of the human adenosine A1-receptor

scientific article published on 3 October 2006

A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A3 receptor

scientific article published on 27 March 2019

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.

scientific article published in November 2017

A novel fluorescent histamine H(1) receptor antagonist demonstrates the advantage of using fluorescence correlation spectroscopy to study the binding of lipophilic ligands

scientific article published on March 2012

A1 adenosine receptor modulation of electrically-evoked contractions in the bisected vas deferens and cauda epididymis of the guinea-pig

scientific article published in July 1998

A1 and A2 adenosine receptor modulation of contractility in the cauda epididymis of the guinea-pig

scientific article published in October 1998

Activation of a metabotropic excitatory amino acid receptor potentiates A2b adenosine receptor-stimulated cyclic AMP accumulation

scientific article published in November 1992

Activation of phospholipase C by G-protein beta gamma subunits in DDT1MF-2 cells.

scientific article

Adenosine A1 receptor-mediated inhibition of cyclic AMP accumulation in type-2 but not type-1 rat astrocytes

scientific article published on 01 June 1996

Adenosine-A3 receptors in neutrophil microdomains promote the formation of bacteria-tethering cytonemes

scientific article

Adenylyl cyclase AC8 directly controls its micro-environment by recruiting the actin cytoskeleton in a cholesterol-rich milieu.

scientific article published on February 2012

Agonist actions of "beta-blockers" provide evidence for two agonist activation sites or conformations of the human beta1-adrenoceptor

scientific article published in June 2003

Agonist and inverse agonist actions of beta-blockers at the human beta 2-adrenoceptor provide evidence for agonist-directed signaling

scientific article published on December 2003

Agonist-induced changes in [Ca2+]i in N1E-115 cells: differential effects of bradykinin and carbachol

scientific article

Agonist-occupied A3 adenosine receptors exist within heterogeneous complexes in membrane microdomains of individual living cells.

scientific article

Allosteric interactions across native adenosine-A3 receptor homodimers: quantification using single-cell ligand-binding kinetics

scientific article

Allosteric interactions at adenosine A(1) and A(3) receptors: new insights into the role of small molecules and receptor dimerization

scientific article published on March 2014

Alpha- and beta-adrenoceptor regulation of cyclic AMP accumulation in cultured rat astrocytes. A comparison of primary protoplasmic and mixed fibrous/protoplasmic astroglial cultures

scientific article published on 01 June 1991

An endogenous A2B adenosine receptor coupled to cyclic AMP generation in human embryonic kidney (HEK 293) cells

scientific article published in October 1997

Antagonism of central histamine H1 receptors by antipsychotic drugs

scientific article published on December 1978

Antagonist selective modulation of adenosine A1 and A3 receptor pharmacology by the food dye Brilliant Black BN: evidence for allosteric interactions

scientific article

Application of BRET to monitor ligand binding to GPCRs

scientific article

Beta-adrenoceptor-mediated inhibition of alpha 1-adrenoceptor-mediated and field stimulation-induced contractile responses in the prostate of the guinea pig.

scientific article published on November 1997

Binding kinetics of ligands acting at GPCRs

scientific article published on 08 February 2019

Biophysical Detection of Diversity and Bias in GPCR Function

scientific article published on 05 March 2014

Bradykinin B2- and 5-hydroxytryptamine (5-HT2)-receptor stimulated increases in intracellular calcium in cultured guinea-pig aortic smooth muscle cells

scientific article published on 01 March 1994

CRISPR-Mediated Protein Tagging with Nanoluciferase to Investigate Native Chemokine Receptor Function and Conformational Changes

scientific article published on 07 February 2020

CXCL17 is an allosteric inhibitor of CXCR4 through a mechanism of action involving glycosaminoglycans

scientific article published in 2024

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.

scientific article

Characteristics of [3H]mepyramine binding in DDT1MF-2 cells: evidence for high affinity binding to a functional histamine H1 receptor.

scientific article published on July 1994

Characterization of isoprenaline- and salmeterol-stimulated interactions between beta2-adrenoceptors and beta-arrestin 2 using beta-galactosidase complementation in C2C12 cells

scientific article

Clathrin-independent internalization of the human histamine H1-receptor in CHO-K1 cells

scientific article published on October 2005

Community guidelines for GPCR ligand bias: IUPHAR review 32

Comparison of potassium currents in human decidua before and after the onset of labor

scientific article published on 22 January 2003

Comparison of the ligand-binding properties of fluorescent VEGF-A isoforms to VEGF receptor 2 in living cells and membrane preparations using NanoBRET

scientific article published on 15 July 2019

Conversion of a non-selective adenosine receptor antagonist into A3-selective high affinity fluorescent probes using peptide-based linkers.

scientific article published in September 2013

Coupling of the human A1 adenosine receptor to different heterotrimeric G proteins: evidence for agonist-specific G protein activation

scientific article published on 9 August 2004

Cross-talk between different receptor-effector systems in the mammalian CNS.

scientific article

Desensitization of muscarinic receptor-coupled inositol phospholipid hydrolysis in human detrusor cultured smooth cells

scientific article published on 01 April 1996

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)

scientific article published on 27 January 2017

Design and use of fluorescent ligands to study ligand-receptor interactions in single living cells

scientific article published in January 2011

Detection of the secondary, low-affinity β1 -adrenoceptor site in living cells using the fluorescent CGP 12177 derivative BODIPY-TMR-CGP.

scientific article published on December 2014

Development of novel fluorescent histamine H1-receptor antagonists to study ligand-binding kinetics in living cells

scientific article

Differential effects of elevated calcium ion concentrations on inositol phospholipid responses in mouse and rat cerebral cortical slices

scientific article

Direct visualisation of internalization of the adenosine A3 receptor and localization with arrestin3 using a fluorescent agonist.

scientific article published on 30 April 2015

Distribution of receptors mediating phosphoinositide hydrolysis in cultured human umbilical artery smooth muscle and endothelial cells

scientific article published in March 1995

Do polyamines regulate the NMDA inhibition of muscarinic receptor-induced phosphoinositide turnover in guinea pig brain?

scientific article published in October 1991

Effect of CCR5 receptor antagonists on endocytosis of the human CCR5 receptor in CHO-K1 cells

scientific article published on 28 January 2008

Effect of a toggle switch mutation in TM6 of the human adenosine A₃ receptor on Gi protein-dependent signalling and Gi-independent receptor internalization

scientific article published on August 2014

Effects of isozyme selective phosphodiesterase inhibitors on bovine tracheal smooth muscle tone

scientific article published on 01 January 1992

Effects of receptor tyrosine kinase inhibitors on VEGF165 a- and VEGF165 b-stimulated gene transcription in HEK-293 cells expressing human VEGFR2.

scientific article published on 10 April 2015

Expression of beta 2-adrenoceptors mediating cyclic AMP accumulation in astroglial and neuronal cell lines derived from the rat CNS.

scientific article published on November 1990

Expression of muscarinic M3-receptors coupled to inositol phospholipid hydrolysis in human detrusor cultured smooth muscle cells

scientific article published on 01 September 1995

Extended mepyramine treatment and histamine H1-receptors in guinea-pig brain.

scientific article

Fluorescence Approaches Unravel Spatial and Temporal Aspects of GPCR Organisation, Location, and Intracellular Signalling.

scientific article published on 21 December 2017

Fluorescence- and bioluminescence-based approaches to study GPCR ligand binding.

scientific article published on 28 August 2015

Fluorescent ligands for G protein-coupled receptors: illuminating receptor-ligand interactions for drug discovery.

scientific article published in August 2013

Fluorescent ligands: Bringing light to emerging GPCR paradigms

scientific article published on 06 February 2020

Fragment screening at adenosine-A(3) receptors in living cells using a fluorescence-based binding assay

scientific article

Fragment-Based Discovery of Subtype-Selective Adenosine Receptor Ligands from Homology Models

scientific article published on 22 November 2015

G protein-coupled-receptor cross-talk: the fine-tuning of multiple receptor-signalling pathways

scientific article published on 01 March 1998

G-protein-coupled receptors: past, present and future.

scientific article published on January 2006

GPCR signaling: understanding the pathway to successful drug discovery.

scientific article published on January 2009

Gi-Protein alpha-subunit mRNA antisense oligonucleotide inhibition of Gi-coupled receptor contractile activity in the epididymis of the guinea-pig

scientific article

High, stable expression of the bovine histamine H1-receptor coupled to [Ca2+]i mobilisation in CHO-K1 cells

scientific article published on 01 September 1993

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.

scientific article published on 13 February 2012

Histamine H1-agonist potentiation of adenosine-stimulated cyclic AMP accumulation in slices of guinea-pig cerebral cortex: comparison of response and binding parameters

scientific article

Histamine-induced hydrolysis of polyphosphoinositides in guinea-pig ileum and brain

scientific article published in May 1986

Histamine-stimulated increases in intracellular calcium in the smooth muscle cell line, DDT1MF-2.

scientific article published on September 1991

Human 5-HT1B receptor stimulated inositol phospholipid hydrolysis in CHO cells: synergy with Gq-coupled receptors

scientific article published on May 1998

Human adenosine A1 receptor and P2Y2-purinoceptor-mediated activation of the mitogen-activated protein kinase cascade in transfected CHO cells.

scientific article published on August 1998

Identification of key residues in transmembrane 4 responsible for the secondary, low-affinity conformation of the human β1-adrenoceptor

scientific article

Impact of polymorphic variants on the molecular pharmacology of the two-agonist conformations of the human β1-adrenoceptor

scientific article

Influence of agonist efficacy and receptor phosphorylation on antagonist affinity measurements: differences between second messenger and reporter gene responses

scientific article published in September 2003

Influence of fluorophore and linker composition on the pharmacology of fluorescent adenosine A1 receptor ligands

scientific article

Influence of rolipram on the cyclic 3',5'-adenosine monophosphate response to histamine and adenosine in slices of guinea-pig cerebral cortex

scientific article

Inhibition by H1-antihistamines of the uptake of noradrenaline and 5-HT into rat brain synaptosomes

scientific article

Inhibition of tissue transglutaminase 2 attenuates contractility of pregnant human myometrium

scientific article published on 01 December 2010

Insights into GPCR pharmacology from the measurement of changes in intracellular cyclic AMP; advantages and pitfalls of differing methodologies

scientific article

Interactions between adenosine A1- and histamine H1-receptors.

scientific article published on August 1994

Involvement of G-protein βγ subunits in coupling the adenosine A1 receptor to phospholipase C in transfected CHO cells ⬇️

scientific article published on August 14, 1998

Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism

scientific article published on 26 June 2014

Ligand Residence Time at G-protein-Coupled Receptors-Why We Should Take Our Time To Study It.

scientific article published on 07 July 2015

Ligand-directed covalent labelling of a GPCR with a fluorescent tag in live cells

scientific article published on 27 November 2020

Mathematical modelling of signalling in a two-ligand G-protein coupled receptor system: agonist-antagonist competition

scientific article published on 20 November 2009

Mechano-sensitivity of β2-adrenoceptors enhances constitutive activation of cAMP generation that is inhibited by inverse agonists

scientific article published in 2024

Modelling of signalling via G-protein coupled receptors: pathway-dependent agonist potency and efficacy

scientific article published in September 2003

Modelling of the activation of G-protein coupled receptors: drug free constitutive receptor activity

scientific article published on 5 April 2009

Modelling the activation of G-protein coupled receptors by a single drug

scientific article published on 26 February 2009

Modulation by cellular cholesterol of gene transcription via the cyclic AMP response element

scientific article

Modulation of carbachol-induced inositol phosphate formation in bovine tracheal smooth muscle by cyclic AMP phosphodiesterase inhibitors

scientific article published on 01 April 1990

Monoclonal anti-β1-adrenergic receptor antibodies activate G protein signaling in the absence of β-arrestin recruitment

scientific article published on January 2014

Multiple GPCR conformations and signalling pathways: implications for antagonist affinity estimates.

scientific article published on 13 July 2007

NanoBRET Approaches to Study Ligand Binding to GPCRs and RTKs.

scientific article published on 10 November 2017

NanoBiT Complementation to Monitor Agonist-Induced Adenosine A1 Receptor Internalization

scientific article published on 04 October 2019

Negative cooperativity across β1-adrenoceptor homodimers provides insights into the nature of the secondary low-affinity CGP 12177 β1-adrenoceptor binding conformation.

scientific article published on 2 April 2015

New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains of single living cells.

scientific article published on 24 January 2007

Nonselective effects of the putative phospholipase C inhibitor, U73122, on adenosine A1 receptor-mediated signal transduction events in Chinese hamster ovary cells

scientific article published on 01 December 1998

Novel selective β1-adrenoceptor antagonists for concomitant cardiovascular and respiratory disease.

scientific article published on 11 April 2017

Oxytocin inhibits T-type calcium current of human decidual stromal cells

scientific article published on 26 April 2005

Pharmacological characterization of CGP 12177 at the human beta(2)-adrenoceptor

scientific article published in October 2002

Pharmacology and direct visualisation of BODIPY-TMR-CGP: a long-acting fluorescent beta2-adrenoceptor agonist

scientific article published on May 2003

Pharmacology under the microscope: the use of fluorescence correlation spectroscopy to determine the properties of ligand-receptor complexes

scientific article

Plasma membrane diffusion of G protein-coupled receptor oligomers

scientific article published on 21 July 2008

Potentiation of adenosine A1 receptor-mediated inositol phospholipid hydrolysis by tyrosine kinase inhibitors in CHO cells

scientific article published on November 1998

Predicting in vivo cardiovascular properties of β-blockers from cellular assays: a quantitative comparison of cellular and cardiovascular pharmacological responses.

scientific article

Probe dependence of allosteric enhancers on the binding affinity of adenosine A -receptor agonists at rat and human A -receptors measured using NanoBRET

scientific article published on 06 March 2019

Probing the binding of interleukin-23 to individual receptor components and the IL-23 heteromeric receptor complex in living cells using NanoBRET

scientific article published on 25 May 2021

Probing the pharmacology of G protein-coupled receptors with fluorescent ligands.

scientific article published on 13 May 2015

Qualitative differences in [Ca2+]i increases and InsP3 generation following stimulation of N1E-115 cells with micromolar and millimolar ATP.

scientific article published on October 1992

Quantitative analysis of neuropeptide Y receptor association with beta-arrestin2 measured by bimolecular fluorescence complementation.

scientific article

Quantitative profiling of nucleotides and related phosphate-containing metabolites in cultured mammalian cells by liquid chromatography tandem electrospray mass spectrometry

scientific article published on 15 July 2008

Real-Time Ligand Binding of Fluorescent VEGF-A Isoforms that Discriminate between VEGFR2 and NRP1 in Living Cells

scholarly article by Chloe J Peach published in October 2018

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

scientific article

Receptor-stimulated phospholipase C activity in human umbilical artery cultured endothelial cells grown in a low oxygen environment

scientific article published on 01 December 1997

Reporter-gene systems for the study of G-protein-coupled receptors.

scientific article

Role of key transmembrane residues in agonist and antagonist actions at the two conformations of the human beta1-adrenoceptor.

scientific article published on 7 August 2008

Salmeterol's extreme β2 selectivity is due to residues in both extracellular loops and transmembrane domains.

scientific article published on 16 October 2014

Selective potentiation of histamine H1-receptor stimulated calcium responses by 1,4-dithiothreitol in DDT1MF-2 cells

scientific article published on November 1994

Sensitivity of histamine H3 receptor agonist-stimulated [35S]GTP gamma[S] binding to pertussis toxin

scientific article published in January 1996

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

scientific article published on 19 May 2020

Specific binding of 3H-mepyramine to histamine H1 receptors in intestinal smooth muscle

scientific article

Structure-Activity Relationships of the Sustained Effects of Adenosine A2A Receptor Agonists Driven by Slow Dissociation Kinetics.

scientific article published on November 2016

Studies on the mechanism of histamine-induced release of noradrenaline and 5-hydroxytryptamine from slices of rat cerebral cortex.

scientific article

Studying GPCR Pharmacology in Membrane Microdomains: Fluorescence Correlation Spectroscopy Comes of Age.

scientific article published on 22 December 2017

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

scientific article published on 18 May 2021

Synergistic interactions between human transfected adenosine A1 receptors and endogenous cholecystokinin receptors in CHO cells

scientific article published on 01 April 1996

Synthesis and Evaluation of the First Fluorescent Antagonists of the Human P2Y2 Receptor Based on AR-C118925.

scientific article published on 20 March 2018

Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors.

scientific article published on 16 September 2011

Synthesis and in vitro and in vivo characterization of highly β1-selective β-adrenoceptor partial agonists.

scientific article published on 10 May 2013

Temporal characteristics of cAMP response element-mediated gene transcription: requirement for sustained cAMP production

scientific article published in April 2004

The control of intracellular calcium and neurotransmitter release in guinea pig-derived cerebral cortical synaptoneurosomes

scientific article published in January 1993

The effect of two selective A1 -receptor agonists and the bitopic ligand VCP746 on heart rate and regional vascular conductance in conscious rats

scientific article published on 01 January 2020

The effects of beta-phorbol-12,13 dibutyrate on agonist-induced increases in [Ca2+]i in N1E-115 cells. Differential modulation of responses to angiotensin II and bradykinin

scientific article published on 01 February 1993

The evolving small-molecule fluorescent-conjugate toolbox for Class A GPCRs

scientific article

The growth response of Escherichia coli to neurotransmitters and related catecholamine drugs requires a functional enterobactin biosynthesis and uptake system

scientific article published on November 2002

The nature of the binding of [3H]mepyramine to homogenates of guinea-pig cerebral cortex at different [3H]ligand concentrations

scientific article published in August 1983

The ups and downs of Gs- to Gi-protein switching

scientific article published in April 2003

The use of fluorescence correlation spectroscopy to characterize the molecular mobility of fluorescently labelled G protein-coupled receptors

scientific article published on April 2016

Transfected adenosine A1 receptor-mediated modulation of thrombin-stimulated phospholipase C and phospholipase A2 activity in CHO cells

scientific article published on 01 February 1997

Transgenic enrichment of cardiomyocytes from human embryonic stem cells

scientific article

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

scientific article

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.

scientific article

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