Research Repository

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Micro-pharmacokinetics: quantifying local drug concentration at live cell membranes (2018)
Journal Article
Gherbi, K., Briddon, S. J., & Charlton, S. J. (in press). Micro-pharmacokinetics: quantifying local drug concentration at live cell membranes. Scientific Reports, 8, doi:10.1038/s41598-018-21100-x. ISSN 2045-2322

Fundamental equations for determining pharmacological parameters, such as the binding afnity of a ligand for its target receptor, assume a homogeneous distribution of ligand, with concentrations in the immediate vicinity of the receptor being the sam... Read More

Development of novel fluorescent histamine H₁-receptor antagonists to study ligand-binding kinetics in living cells (2018)
Journal Article
antagonists to study ligand-binding kinetics in living cells. Scientific Reports, 8, doi:10.1038/s41598-018-19714-2. ISSN 2045-2322

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

Fluorescently labeled morphine derivatives for bioimaging studies (2018)
Journal Article
Lam, R., Gondin, A. B., Canals, M., Kellam, B., Briddon, S. J., Graham, B., & Scammells, P. J. (2018). Fluorescently labeled morphine derivatives for bioimaging studies. Journal of Medicinal Chemistry, 61(3), doi:10.1021/acs.jmedchem.7b01811

Opioids, like morphine, are the mainstay analgesics for the treatment and control of pain. Despite this, they often exhibit severe side effects that limit dose; patients often become tolerant and dependent on these drugs, which remains a major health... Read More

Synthesis, biological evaluation, and utility of fluorescent ligands targeting the μ-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 μ-opioid receptor. Journal of Medicinal Chemistry, 58(24), doi: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

Adenosine-A3 receptors in neutrophil microdomains promote the formation of bacteria-tethering cytonemes (2013)
Journal Article
promote the formation of bacteria-tethering cytonemes. EMBO Reports, 14(8), doi:10.1038/embor.2013.89. ISSN 1469-221X

The A3‐adenosine receptor (A3AR) has recently emerged as a key regulator of neutrophil behaviour. Using a fluorescent A3AR ligand, we show that A3ARs aggregate in highly polarized immunomodulatory microdomains on human neutrophil membranes. In additi... Read More

Fluorescence correlation spectroscopy, combined with bimolecular fluorescence complementation, reveals the effects of β-arrestin complexes and endocytic targeting on the membrane mobility of neuropeptide Y receptors (2012)
Journal Article
on the membrane mobility of neuropeptide Y receptors. Biochimica et Biophysica Acta (BBA) - Molecular Cell Research, 1823(6), ISSN 0167-4889

Fluorescence correlation spectroscopy (FCS) and photon counting histogram (PCH) analysis are powerful ways to study mobility and stoichiometry of G protein coupled receptor complexes, within microdomains of single living cells. However, relating thes... Read More