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All Outputs (4)

Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the ?-Opioid Receptor (2015)
Journal Article
Schembri, L. S., Stoddart, L. A., Briddon, S. J., Kellam, B., Canals, M., Graham, B., & Scammells, P. J. (2015). Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the ?-Opioid Receptor. Journal of Medicinal Chemistry, 58(24), 9754-9767. https://doi.org/10.1021/acs.jmedchem.5b01664

Fluorescently labeled ligands are useful pharmacological research tools for studying receptor localization, trafficking, and signaling processes via fluorescence imaging. They are also employed in fluorescent binding assays. This study is centered on... Read More about Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the ?-Opioid Receptor.

Antitumour benzothiazoles. Part 32: DNA adducts and double strand breaks correlate with activity; synthesis of 5F203 hydrogels for local delivery (2015)
Journal Article
Stone, E. L., Citossi, F., Singh, R., Kaur, B., Gaskell, M., Farmer, P. B., …Bradshaw, T. D. (2015). Antitumour benzothiazoles. Part 32: DNA adducts and double strand breaks correlate with activity; synthesis of 5F203 hydrogels for local delivery. Bioorganic and Medicinal Chemistry, 23(21), 6891-6899. https://doi.org/10.1016/j.bmc.2015.09.052

Potent, selective antitumour AhR ligands 5F 203 and GW 610 are bioactivated by CYPs 1A1 and 2W1. Herein we reason that DNA adducts’ generation resulting in lethal DNA double strand breaks (DSBs) underlies benzothiazoles’ activity. Treatment of sensit... Read More about Antitumour benzothiazoles. Part 32: DNA adducts and double strand breaks correlate with activity; synthesis of 5F203 hydrogels for local delivery.

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.

Synthesis of new DPP-4 inhibitors based on a novel tricyclic scaffold (2015)
Journal Article
Schwehm, C., Li, J., Song, H., Hu, X., Kellam, B., & Stocks, M. (2015). Synthesis of new DPP-4 inhibitors based on a novel tricyclic scaffold. ACS Medicinal Chemistry Letters, 6(3), https://doi.org/10.1021/ml500503n

A novel molecular scaffold has been synthesized and its synthesis and incorporation into new analogues of biologically active molecules will be discussed. A comparison of the inhibitory activity of these compounds to the known type-2 diabetes compoun... Read More about Synthesis of new DPP-4 inhibitors based on a novel tricyclic scaffold.