Dr STEPHEN BRIDDON's Outputs (4)

Structure-based exploration and pharmacological evaluation of N-substituted piperidin-4-yl-methanamine CXCR4 chemokine receptor antagonists (2018)
Journal Article
Adlere, I., Sun, S., Zarca, A., Roumen, L., Gozelle, M., Viciano, C. P., Caspar, B., Arimont, M., Bebelman, J., Briddon, S., Hoffmann, C., Hill, S., Smit, M., Vischer, H., Wijtmans, M., de Graaf, C., de Esch, I., & Leurs, R. (2019). Structure-based exploration and pharmacological evaluation of N-substituted piperidin-4-yl-methanamine CXCR4 chemokine receptor antagonists. European Journal of Medicinal Chemistry, 162, 631-649. https://doi.org/10.1016/j.ejmech.2018.10.060

Using the available structural information of the chemokine receptor CXCR4, we present hit finding and hit exploration studies that make use of virtual fragment screening, design, synthesis and structure-activity relationship (SAR) studies. Fragment... Read More about Structure-based exploration and pharmacological evaluation of N-substituted piperidin-4-yl-methanamine CXCR4 chemokine receptor antagonists.

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, Article 3479. https://doi.org/10.1038/s41598-018-21100-x

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 about Micro-pharmacokinetics: quantifying local drug concentration at live cell membranes.

Development of novel fluorescent histamine H₁-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., Vischer, H. F., Leurs, R., Briddon, S. J., Kellam, B., & 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 H₁-receptor antagonists to study ligand-binding kinetics in living cells.

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), 1316-1329. https://doi.org/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 about Fluorescently Labeled Morphine Derivatives for Bioimaging Studies.