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2018

Conroy, Sean, Kindon, Nicholas, Glenn, Jacqueline, Stoddart, Leigh A., Lewis, Richard James, Hill, Stephen J., Kellam, Barrie and Stocks, Michael J. (2018) Synthesis and evaluation of the first fluorescent antagonists of the human P2Y2 receptor based on AR-C118925. Journal of Medicinal Chemistry, 61 (7). pp. 3089-3113. ISSN 1520-4804

Peach, Chloe J., Kilpatrick, Laura E., Friedman-Ohana, Rachel, Zimmerman, Kris, Robers, Matthew B., Wood, Keith V., Woolard, Jeanette and Hill, Stephen J. (2018) Real-time ligand binding of fluorescent VEGF-A isoforms that discriminate between VEGFR2 and NRP1 in living cells. Cell Chemical Biology . ISSN 2451-9456 (In Press)

Soave, Mark, Cseke, Gabriella, Hutchings, Catherine J., Brown, Alastair J.H., Woolard, Jeanette and Hill, Stephen J. (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 1- adrenoceptors expressed in stable cell lines. Biochemical Pharmacology, 147 . pp. 38-54. ISSN 1873-2968

Stoddart, Leigh A., Vernall, Andrea J., Bouzo-Lorenzo, Monica, Bosma, Reggie, Kooistra, Albert J., de Graaf, Chris, Vischer, Henry F., Leurs, Rob, Briddon, Stephen J., Kellam, Barrie and Hill, Stephen J. (2018) Development of novel fluorescent histamine H₁-receptor antagonists to study ligand-binding kinetics in living cells. Scientific Reports, 8 . p. 1572. ISSN 2045-2322

Goulding, Joelle, May, Lauren T. and Hill, Stephen J. (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. Biochemical Pharmacology, 147 . pp. 55-66. ISSN 1873-2968

2017

Arruda, Maria Augusta, Stoddart, Leigh A., Gherbi, Karolina, Briddon, Stephen J., Kellam, Barrie and Hill, Stephen J. (2017) A non-imaging high throughput approach to chemical library screening at the unmodified adenosine-A3 receptor in living cells. Frontiers in Pharmacology, 8 (908). pp. 1-13. ISSN 1663-9812

Baker, Jillian G., Gardiner, Sheila M., Woolard, Jeanette, Fromont, Christophe, Jadhav, Gopal P., Mistry, Shailesh N., Thompson, Kevin S.J., Kellam, Barrie, Hill, Stephen J. and Fischer, Peter M. (2017) Novel selective β1-adrenoceptor antagonists for concomitant cardiovascular and respiratory disease. FASEB Journal, 31 (7). pp. 3150-3166. ISSN 1530-6860

Kilpatrick, Laura E., Friedman-Ohana, Rachel, Alcobia, Diana C., Riching, Kristin, Peach, Chloe J., Wheal, Amanda J., Briddon, Stephen J., Robers, Matthew B., Zimmerman, Kris, Machleidt, Thomas, Wood, Keith V., Woolard, Jeanette and Hill, Stephen J. (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. Biochemical Pharmacology . ISSN 1873-2968 (In Press)

Schwehm, Carolin, Kellam, Barrie, Garces, Aimie, Hill, Stephen J., Kindon, Nicholas, Bradshaw, Tracey D., Li, Jin, Macdonald, Simon J.F., Rowedder, James E., Stoddart, Leigh A. and Stocks, Michael (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. Journal of Medicinal Chemistry, 60 (4). pp. 1534-1554. ISSN 1520-4804

Hothersall, J. Daniel, Guo, Dong, Sarda, Sunil, Sheppard, Robert J., Chen, Hongming, Keur, Wesley, Waring, Michael J., IJzerman, Adriaan P., Hill, Stephen J., Dale, Ian L. and Rawlins, Philip B. (2017) Structure-activity relationships of the sustained effects of adenosine A2A receptor agonists driven by slow dissociation kinetics. Molecular Pharmacology, 91 (1). pp. 25-38. ISSN 1521-0111

2016

Soave, Mark, Stoddart, Leigh A., Brown, Alastair, Woolard, Jeanette and Hill, Stephen J. (2016) 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. Pharmacology Research and Perspectives, 4 (5). e00250/1-e00250/13. ISSN 2052-1707

Kilpatrick, Laura E. and Hill, Stephen J. (2016) The use of fluorescence correlation spectroscopy to characterize the molecular mobility of fluorescently labelled G protein-coupled receptors. Biochemical Society Transactions, 44 (2). pp. 624-629. ISSN 0300-5127

2015

Ranganathan, Anirudh, Stoddart, Leigh A., Hill, Stephen J. and Carlsson, Jens (2015) Fragment-based discovery of subtype-selective adenosine receptor ligands from homology models. Journal of Medicinal Chemistry, 58 (24). pp. 9578-9590. ISSN 1520-4804

Blaxter, L.L., Morris, David E., Crowe, John A., Henry, C., Hill, Stephen J., Sharkey, Don, Vyas, H. and Hayes-Gill, Barrie R. (2015) An automated quasi-continuous capillary refill timing device. Physiological Measurement, 37 (1). ISSN 1361-6579

Stoddart, Leigh A., Vernall, Andrea J., Briddon, Stephen J., Kellam, Barrie and Hill, Stephen J. (2015) Direct visualisation of internalization of the adenosine A3 receptor and localization with arrestin3 using a fluorescent agonist. Neuropharmacology, 98 . pp. 68-77. ISSN 1873-7064

Gherbi, Karolina, May, Lauren T., Baker, Jillian G., Briddon, Stephen J. and Hill, Stephen J. (2015) Negative cooperativity across 1-adrenoceptor homodimers provides insights into the nature of the secondary low-affinity CGP 12177 1-adrenoceptor binding conformation. FASEB Journal, 29 (7). pp. 2859-2871. ISSN 1530-6860

Stoddart, Leigh A., Johnstone, Elizabeth K.M., Wheal, Amanda J., Goulding, Joelle, Robers, Matthew B., Machleidt, Thomas, Wood, Keith V., Hill, Stephen J. and Pfleger, Kevin D.G. (2015) Application of BRET to monitor ligand binding to GPCRs. Nature Methods, 12 . pp. 661-663. ISSN 1548-7105

Carter, Joanne J., Wheal, Amanda J., Hill, Stephen J. and Woolard, Jeanette (2015) Effects of receptor tyrosine kinase inhibitors on VEGF165a- and VEGF165b-stimulated gene transcription in HEK-293 cells expressing human VEGFR2. British Journal of Pharmacology, 172 (12). pp. 3141-3150. ISSN 1476-5381

Baker, Jillian G., Proudman, Richard G.W. and Hill, Stephen J. (2015) Salmeterol's extreme b2 selectivity is due to residues in both extracellular loops and transmembrane domains. Molecular Pharmacology, 87 (1). pp. 103-120. ISSN 1521-0111

2014

Corriden, Ross, Kilpatrick, Laura E., Kellam, Barrie, Briddon, Stephen J. and Hill, Stephen J. (2014) Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism. FASEB Journal, 28 (10). pp. 4211-4222. ISSN 1530-6860

Stoddart, Leigh A., Kellam, Barrie, Briddon, Stephen J. and Hill, Stephen J. (2014) Effect of a toggle switch mutation in TM6 of the human adenosine A3 receptor on Gi protein-dependent signalling and Gi-independent receptor internalization. British Journal of Pharmacology, 171 (16). pp. 3827-3844. ISSN 0007-1188

Baker, Jillian G., Proudman, Richard G.W. and Hill, Stephen J. (2014) Identification of key residues in transmembrane 4 responsible for the secondary, low-affinity conformation of the human 1-adrenoceptor. Molecular Pharmacology, 85 (5). pp. 811-829. ISSN 1521-0111

Hill, Stephen J., May, Lauren T., Kellam, Barrie and Woolard, Jeanette (2014) Allosteric interactions at adenosine A1 and A3 receptors: new insights into the role of small molecules and receptor dimerization. British Journal of Pharmacology, 171 (5). pp. 1102-1113. ISSN 0007-1188

Vernall, Andrea J., Hill, Stephen J. and Kellam, Barrie (2014) The evolving small-molecule fluorescent-conjugate toolbox for Class A GPCRs. British Journal of Pharmacology, 171 (5). pp. 1073-1084. ISSN 0007-1188

2013

Hutchings, Catherine J., Cseke, Gabriella, Osborne, Greg, Woolard, Jeanette, Zhukov, Andrei, Koglin, Markus, Jazayeri, Ali, Pandya-Pathak, Jahnavi, Langmead, Christopher J., Hill, Stephen J., Weir, Malcolm and Marshall, Fiona H. (2013) Monoclonal anti-β1-adrenergic receptor antibodies activate G protein signaling in the absence of β-arrestin recruitment. mAbs, 6 (1). pp. 246-261. ISSN 1942-0870

Baker, Jillian G., Hill, Stephen J. and Proudman, Richard G.W. (2013) Impact of polymorphic variants on the molecular pharmacology of the two-agonist conformations of the human β1-adrenoceptor. PLoS ONE, 8 (11). ISSN 1932-6203

Vernall, Andrea J., Stoddart, Leigh A., Briddon, Stephen J., Ng, Hui Wen, Laughton, Charles A., Doughty, Stephen W., Hill, Stephen J. and Kellam, Barrie (2013) Conversion of a non-selective adenosine receptor antagonist into A3-selective high affinity fluorescent probes using peptide-based linkers. Organic & Biomolecular Chemistry, 11 (34). pp. 5673-5682. ISSN 1477-0520

Corriden, Ross, Self, Tim, Akong-Moore, Kathryn, Nizet, Victor, Kellam, Barrie, Briddon, Stephen J. and Hill, Stephen J. (2013) Adenosine-A3 receptors in neutrophil microdomains promote the formation of bacteria-tethering cytonemes. EMBO reports, 14 (8). pp. 726-732. ISSN 1469-221X

Mistry, Shailesh N., Baker, Jillian G., Fischer, Peter M., Hill, Stephen J., Gardiner, Sheila M. and Kellam, Barrie (2013) Synthesis and in vitro and in vivo characterization of highly β1-Selective β-Adrenoceptor partial agonists. Journal of Medicinal Chemistry, 56 (10). pp. 3852-3865. ISSN 0022-2623

2012

Baker, Jillian G., Mistry, Shailesh N., Fischer, Peter M., Hill, Stephen J., Gardiner, Sheila M. and Kellam, Barrie (2012) In vitro and in vivo analysis of a novel highly selective β1-adrenoceptor partial agonist. In: British Pharmacological Society 4th Focused Meeting on Cell Signalling, 23-24 April 2012, Leicester, UK.

2011

Baker, Jillian G., Kemp, Philip, March, Julie, Fretwell, Laurice, Hill, Stephen J. and Gardiner, Sheila M. (2011) Predicting in vivo cardiovascular properties of β-blockers from cellular assays: a quantative comparison of cellular and cardiovascular pharmacological responses. FASEB Journal, 25 (12). pp. 4486-4497. ISSN 0892-6638

Baker, Jillian G., Adams, Luke A., Salchow, Karolina, Mistry, Shailesh N., Middleton, Richard J., Hill, Stephen J. and Kellam, Barrie (2011) Synthesis and characterization of high-affinity 4, 4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors. Journal of Medicinal Chemistry, 54 (19). pp. 6874-6887. ISSN 0022-2623

Baker, Jillian G., Adams, Luke A., Salchow, Karolina, Mistry, Shailesh N., Middleton, Richard J., Hill, Stephen J. and Kellam, Barrie (2011) Synthesis and characterization of high-affinity 4,4-difluoro-4-bora-3a,4a-diaza-s-indacene-labeled fluorescent ligands for human β-adrenoceptors. Journal of Medicinal Chemistry, 54 (19). pp. 6874-6887. ISSN 0022-2623

Baker, Jillian G., Hill, Stephen J. and Summers, Roger J. (2011) Evolution of β-blockers: from anti-anginal drugs to ligand-directed signalling. Trends in Pharmacological Sciences, 32 (4). pp. 227-234. ISSN 0165-6147