Outputs (40)

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.

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.

Preparation and structural analysis of (±)-cis-ethyl 2-sulfanylidenedecahydro-1,6-naphthyridine-6-carboxylate and (±)-trans-ethyl 2-oxooctahydro-1H-pyrrolo[3,2-c]pyridine-5-carboxylate (2014)
Journal Article
Schwehm, C., Lewis, W., Blake, A. J., Kellam, B., & Stocks, M. J. (2014). Preparation and structural analysis of (±)-cis-ethyl 2-sulfanylidenedecahydro-1,6-naphthyridine-6-carboxylate and (±)-trans-ethyl 2-oxooctahydro-1H-pyrrolo[3,2-c]pyridine-5-carboxylate. Acta Crystallographica Section C: Structural Chemistry, 70(12), 1161-1168. https://doi.org/10.1107/s205322961402436x

Bicycle ring closure on a mixture of (4aS,8aR)- and (4aR,8aS)-ethyl 2-oxodecahydro-1,6-naphthyridine-6-carboxylate, followed by conversion of the separated cis and trans isomers to the corresponding thioamide derivatives, gave (4aSR,8aRS)-ethyl 2-sul... Read More about Preparation and structural analysis of (±)-cis-ethyl 2-sulfanylidenedecahydro-1,6-naphthyridine-6-carboxylate and (±)-trans-ethyl 2-oxooctahydro-1H-pyrrolo[3,2-c]pyridine-5-carboxylate.

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.

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.

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.

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.

Synthesis and in vitro and in vivo characterization of highly ?1-Selective ?-Adrenoceptor partial agonists (2013)
Journal Article
Mistry, S. N., Baker, J. G., Fischer, P. M., Hill, S. J., Gardiner, S. M., & Kellam, B. (2013). Synthesis and in vitro and in vivo characterization of highly ?1-Selective ?-Adrenoceptor partial agonists. Journal of Medicinal Chemistry, 56(10), https://doi.org/10.1021/jm400348g

β-Adrenoceptor antagonists boast a 50-year use for symptomatic control in numerous cardiovascular diseases. One might expect highly selective antagonists are available for the human β-adrenoceptor subtype involved in these diseases, yet few truly β1-... Read More about Synthesis and in vitro and in vivo characterization of highly ?1-Selective ?-Adrenoceptor partial agonists.

In vitro and in vivo analysis of a novel highly selective ?1-adrenoceptor partial agonist. (2012)
Conference Proceeding
Baker, J. G., Mistry, S. N., Fischer, P. M., Hill, S. J., Gardiner, S. M., & Kellam, B. (2012). In vitro and in vivo analysis of a novel highly selective ?1-adrenoceptor partial agonist.