All Outputs (32)

Developing a self-healing supramolecular nucleoside hydrogel (2016)
Journal Article
Skilling, K. J., Kellam, B., Ashford, M., Bradshaw, T. D., & Marlow, M. (2016). Developing a self-healing supramolecular nucleoside hydrogel. Soft Matter, 12(43), 8950-8957. https://doi.org/10.1039/c6sm01779g

© 2016 The Royal Society of Chemistry. Low molecular weight gelator hydrogels provide a viable alternative to traditional polymer based drug delivery platforms, owing to their tunable stability and in most cases inherent biocompatibility. Here we rep... Read More about Developing a self-healing supramolecular nucleoside hydrogel.

Drug-like antagonists of P2Y receptors — from lead identification to drug development (2016)
Journal Article
Conroy, S., Kindon, N., Kellam, B., & Stocks, M. (in press). Drug-like antagonists of P2Y receptors — from lead identification to drug development. Journal of Medicinal Chemistry, https://doi.org/10.1021/acs.jmedchem.5b01972

P2Y receptors are expressed in virtually all cells and tissue types and mediate an astonishing array of biological functions, including platelet aggregation, smooth muscle cell proliferation, and immune regulation. The P2Y receptors belong to the G p... Read More about Drug-like antagonists of P2Y receptors — from lead identification to drug development.

Alkylation of staurosporine to derive a kinase probe for fluorescence applications (2016)
Journal Article
Disney, A. J., Kellam, B., & Dekker, L. V. (in press). Alkylation of staurosporine to derive a kinase probe for fluorescence applications. ChemMedChem, 11, https://doi.org/10.1002/cmdc.201500589

The natural product staurosporine is a high-affinity inhibitor of nearly all mammalian protein kinases.The labelling of staurosporine has proven effective as a means of generating protein kinase research tools. Most tools have been generated by acyla... Read More about Alkylation of staurosporine to derive a kinase probe for fluorescence applications.

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), 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 μ-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.

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.

Gelation properties of self-assembling N-acyl modified cytidine derivatives (2014)
Journal Article
Skilling, K. J., Ndungu, A., Kellam, B., Ashford, M., Bradshaw, T. D., & Marlow, M. (in press). Gelation properties of self-assembling N-acyl modified cytidine derivatives. Journal of Materials Chemistry B, 2(47), https://doi.org/10.1039/C4TB01375A

In this study we report the synthesis of new cytidine derived gelators possessing acyl chains of different lengths. These low molecular weight gelators were shown to form self-supporting gels at 0.5 % (w/v) in binary systems of aqueous miscible polar... Read More about Gelation properties of self-assembling N-acyl modified cytidine derivatives.

Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism (2014)
Journal Article
Corriden, R., Kilpatrick, L. E., Kellam, B., Briddon, S. J., & Hill, S. 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), 4211-4222. https://doi.org/10.1096/fj.13-247270

© The Author(s). In our previous work, using a fluorescent adenosine-A3 receptor (A3AR) agonist and fluorescence correlation spectroscopy (FCS), we demonstrated highaffinity labeling of the active receptor (R∗) conformation. In the current study, we... Read More about Kinetic analysis of antagonist-occupied adenosine-A3 receptors within membrane microdomains of individual cells provides evidence of receptor dimerization and allosterism.

The evolving small-molecule fluorescent-conjugate toolbox for Class A GPCRs (2014)
Journal Article
Vernall, A. J., Hill, S. J., & Kellam, B. (2014). The evolving small-molecule fluorescent-conjugate toolbox for Class A GPCRs. British Journal of Pharmacology, 171(5), https://doi.org/10.1111/bph.12265

The past decade has witnessed fluorescently tagged drug molecules gaining significant attraction in their use as pharmacological tools with which to visualize and interrogate receptor targets at the single-cell level. Additionally, one can generate d... Read More about The evolving small-molecule fluorescent-conjugate toolbox for Class A GPCRs.

Allosteric interactions at adenosine A1 and A3 receptors: new insights into the role of small molecules and receptor dimerization (2014)
Journal Article
Hill, S. J., May, L. T., Kellam, B., & Woolard, J. (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), https://doi.org/10.1111/bph.12345

Keywords:adenosine;allosterism;receptor;GPCR;dimerization;biased signalling The purine nucleoside adenosine is present in all cells in tightly regulated concentrations. It is released under a variety of physiological and pathophysiological condition... Read More about Allosteric interactions at adenosine A1 and A3 receptors: new insights into the role of small molecules and receptor dimerization.

Conversion of a non-selective adenosine receptor antagonist into A 3-selective high affinity fluorescent probes using peptide-based linkers (2013)
Journal Article
Vernall, A. J., Stoddart, L. A., Briddon, S. J., Ng, H. W., Laughton, C. A., Doughty, S. W., …Kellam, B. (2013). Conversion of a non-selective adenosine receptor antagonist into A 3-selective high affinity fluorescent probes using peptide-based linkers. Organic and Biomolecular Chemistry, 11(34), 5673-5682. https://doi.org/10.1039/c3ob41221k

Advances in fluorescence-based imaging technologies have helped propel the study of real-time biological readouts and analysis across many different areas. In particular the use of fluorescent ligands as chemical tools to study proteins such as G pro... Read More about Conversion of a non-selective adenosine receptor antagonist into A 3-selective high affinity fluorescent probes using peptide-based linkers.

Adenosine-A3 receptors in neutrophil microdomains promote the formation of bacteria-tethering cytonemes (2013)
Journal Article
Corriden, R., Self, T., Akong-Moore, K., Nizet, V., Kellam, B., Briddon, S. J., & Hill, S. J. (2013). Adenosine-A3 receptors in neutrophil microdomains promote the formation of bacteria-tethering cytonemes. EMBO Reports, 14(8), https://doi.org/10.1038/embor.2013.89

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 about Adenosine-A3 receptors in neutrophil microdomains promote the formation of bacteria-tethering cytonemes.