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Synthesis and evaluation of the first fluorescent antagonists of the human P2Y2 receptor based on AR-C118925 (2018)
Journal Article
Conroy, S., Kindon, N., Glenn, J., Stoddart, L. A., Lewis, R. J., Hill, S. J., …Stocks, M. 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), https://doi.org/10.1021/acs.jmedchem.8b00139

The human P2Y2 receptor (hP2Y2R) is a G protein-coupled receptor that shows promise as a therapeutic target for many important conditions including anti-metastatic cancer therapy and more recently for the treatment of idiopathic pulmonary fibrosis. A... Read More about Synthesis and evaluation of the first fluorescent antagonists of the human P2Y2 receptor based on AR-C118925.

Development of novel fluorescent histamine H?-receptor antagonists to study ligand-binding kinetics in living cells (2018)
Journal Article
Stoddart, L. A., Vernall, A. J., Bouzo-Lorenzo, M., Bosma, R., Kooistra, A. J., de Graaf, C., …Hill, S. J. (2018). Development of novel fluorescent histamine H₁-receptor antagonists to study ligand-binding kinetics in living cells. Scientific Reports, 8, Article 1572. https://doi.org/10.1038/s41598-018-19714-2

The histamine H1-receptor (H1R) is an important mediator of allergy and inflammation. H1R antagonists have particular clinical utility in allergic rhinitis and urticaria. Here we have developed six novel fluorescent probes for this receptor that are... Read More about Development of novel fluorescent histamine H?-receptor antagonists to study ligand-binding kinetics in living cells.

Application of BRET to monitor ligand binding to GPCRs (2015)
Journal Article
Stoddart, L. A., Johnstone, E. K., Wheal, A. J., Goulding, J., Robers, M. B., Machleidt, T., …Pfleger, K. D. (in press). Application of BRET to monitor ligand binding to GPCRs. Nature Methods, 12, https://doi.org/10.1038/nmeth.3398

Bioluminescence resonance energy transfer (BRET) is a well-established method for investigating protein-protein interactions. Here we present a BRET approach to monitor ligand binding to G protein–coupled receptors (GPCRs) on the surface of living ce... Read More about Application of BRET to monitor ligand binding to GPCRs.

Direct visualisation of internalization of the adenosine A3 receptor and localization with arrestin3 using a fluorescent agonist (2015)
Journal Article
Stoddart, L. A., Vernall, A. J., Briddon, S. J., Kellam, B., & Hill, S. J. (2015). Direct visualisation of internalization of the adenosine A3 receptor and localization with arrestin3 using a fluorescent agonist. Neuropharmacology, 98, 68-77. https://doi.org/10.1016/j.neuropharm.2015.04.013

Fluorescence based probes provide a novel way to study the dynamic internalization process of G protein-coupled receptors (GPCRs). Recent advances in the rational design of fluorescent ligands for GPCRs have been used here to generate new fluorescent... Read More about Direct visualisation of internalization of the adenosine A3 receptor and localization with arrestin3 using a fluorescent agonist.

Effect of a toggle switch mutation in TM6 of the human adenosine A3 receptor on Gi protein-dependent signalling and Gi-independent receptor internalization (2014)
Journal Article
Stoddart, L. A., Kellam, B., Briddon, S. J., & Hill, S. 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), https://doi.org/10.1111/bph.12739

Background and Purpose: The highly conserved tryptophan (W6.48) in transmembrane domain 6 of GPCRs has been shown to play a central role in forming an active conformation in response to agonist binding. We set out to characterize the effect of this m... Read More about Effect of a toggle switch mutation in TM6 of the human adenosine A3 receptor on Gi protein-dependent signalling and Gi-independent receptor internalization.