All Outputs (6)

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.

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.

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.

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.

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.