All Outputs (11)

Cannabidiol and fluorinated derivative anti-cancer properties against glioblastoma multiforme cell lines, and synergy with imidazotetrazine agents (2024)
Journal Article
Brookes, A., Kindon, N., Scurr, D. J., Alexander, M. R., Gershkovich, P., & Bradshaw, T. (2024). Cannabidiol and fluorinated derivative anti-cancer properties against glioblastoma multiforme cell lines, and synergy with imidazotetrazine agents. BJC Reports, 2, Article 67. https://doi.org/10.1038/s44276-024-00088-0

Background
Glioblastoma multiforme (GBM) is an aggressive cancer with poor prognosis, partly due to resistance to the standard chemotherapy treatment, temozolomide (TMZ). Phytocannabinoid cannabidiol (CBD) has exhibited anti-cancer effects against G... Read More about Cannabidiol and fluorinated derivative anti-cancer properties against glioblastoma multiforme cell lines, and synergy with imidazotetrazine agents.

Cannabidiol and fluorinated derivative anti-cancer properties against glioblastoma multiforme cell lines, and synergy with imidazotetrazine agents (2024)
Journal Article
Brookes, A., Kindon, N., Scurr, D., Alexander, M., Gershkovich, P., & BRADSHAW, T. (2024). Cannabidiol and fluorinated derivative anti-cancer properties against glioblastoma multiforme cell lines, and synergy with imidazotetrazine agents. British Journal of Cancer, 2, Article 67. https://doi.org/10.1038/s44276-024-00088-0

Background
Glioblastoma multiforme (GBM) is an aggressive cancer with poor prognosis, partly due to resistance to the standard chemotherapy treatment, temozolomide (TMZ). Phytocannabinoid cannabidiol (CBD) has exhibited anti-cancer effects against G... Read More about Cannabidiol and fluorinated derivative anti-cancer properties against glioblastoma multiforme cell lines, and synergy with imidazotetrazine agents.

A novel and selective fluorescent ligand for the study of adenosine A2B receptors (2024)
Journal Article
Patera, F., Mistry, S. J., Kindon, N. D., Comeo, E., Gouding, J., Kellam, B., Kilpatrick, L. E., Franks, H., & Hill, S. J. (2024). A novel and selective fluorescent ligand for the study of adenosine A2B receptors. Pharmacology Research and Perspectives, 12(4), Article e1223. https://doi.org/10.1002/prp2.1223

Fluorescent ligands have proved to be powerful tools in the study of G protein-coupled receptors in living cells. Here we have characterised a new fluorescent ligand PSB603-BY630 that has high selectivity for the human adenosine A2B receptor (A2BR).... Read More about A novel and selective fluorescent ligand for the study of adenosine A2B receptors.

Small-Molecule Fluorescent Ligands for the CXCR4 Chemokine Receptor (2023)
Journal Article
Dekkers, S., Caspar, B., Goulding, J., Kindon, N. D., Kilpatrick, L. E., Stoddart, L. A., …Stocks, M. J. (2023). Small-Molecule Fluorescent Ligands for the CXCR4 Chemokine Receptor. Journal of Medicinal Chemistry, 66(7), 5208-5222. https://doi.org/10.1021/acs.jmedchem.3c00151

The C-X-C chemokine receptor type 4, or CXCR4, is a chemokine receptor found to promote cancer progression and metastasis of various cancer cell types. To investigate the pharmacology of this receptor, and to further elucidate its role in cancer, nov... Read More about Small-Molecule Fluorescent Ligands for the CXCR4 Chemokine Receptor.

Ligand-directed covalent labelling of a GPCR with a fluorescent tag in live cells (2020)
Journal Article
Stoddart, L. A., Kindon, N. D., Otun, O., Harwood, C. R., Patera, F., Veprintsev, D. B., …Kellam, B. (2020). Ligand-directed covalent labelling of a GPCR with a fluorescent tag in live cells. Communications Biology, 3(1), Article 722. https://doi.org/10.1038/s42003-020-01451-w

© 2020, The Author(s). To study the localisation of G protein-coupled receptors (GPCR) in their native cellular environment requires their visualisation through fluorescent labelling. To overcome the requirement for genetic modification of the recept... Read More about Ligand-directed covalent labelling of a GPCR with a fluorescent tag in live cells.

Subtype-Selective Fluorescent Ligands as Pharmacological Research Tools for the Human Adenosine A2A Receptor (2019)
Journal Article
Comeo, E., Kindon, N. D., Soave, M., Stoddart, L. A., Kilpatrick, L. E., Scammells, P. J., …Kellam, B. (2020). Subtype-Selective Fluorescent Ligands as Pharmacological Research Tools for the Human Adenosine A2A Receptor. Journal of Medicinal Chemistry, 63(5), 2656-2672. https://doi.org/10.1021/acs.jmedchem.9b01856

© 2019 American Chemical Society. Among class A G protein-coupled receptors (GPCR), the human adenosine A2A receptor (hA2AAR) remains an attractive drug target. However, translation of A2AAR ligands into the clinic has proved challenging and an impro... Read More about Subtype-Selective Fluorescent Ligands as Pharmacological Research Tools for the Human Adenosine A2A Receptor.

Synthesis and evaluation of the first fluorescent antagonists of the human P2Y2 receptor based on AR-C118925 (2018)
Journal Article
Conroy, S., Kindon, N., Glenn, J., Stoddart, L. A., Lewis, R. J., Hill, S. J., Kellam, B., & Stocks, M. J. (2018). Synthesis and evaluation of the first fluorescent antagonists of the human P2Y2 receptor based on AR-C118925. Journal of Medicinal Chemistry, 61(7), https://doi.org/10.1021/acs.jmedchem.8b00139

The human P2Y2 receptor (hP2Y2R) is a G protein-coupled receptor that shows promise as a therapeutic target for many important conditions including anti-metastatic cancer therapy and more recently for the treatment of idiopathic pulmonary fibrosis. A... Read More about Synthesis and evaluation of the first fluorescent antagonists of the human P2Y2 receptor based on AR-C118925.

From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor (2017)
Journal Article
Kindon, N., Davis, A., Dougall, I., Dixon, J., Johnson, T., Walters, I., …Stocks, M. (2017). From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor. Bioorganic and Medicinal Chemistry Letters, 27(21), 4849-4853. https://doi.org/10.1016/j.bmcl.2017.09.043

The G protein-coupled P2Y2 receptor, activated by ATP and UTP has been reported as a potential drug target for a wide range of important clinical conditions, such as tumor metastasis, kidney disorders, and in the treatment of inflammatory conditions.... Read More about From UTP to AR-C118925, the discovery of a potent non nucleotide antagonist of the P2Y2 receptor.

Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists (2017)
Journal Article
Kindon, N., Andrews, G., Baxter, A., Cheshire, D., Hemsley, P., Johnson, T., …Stocks, M. J. (in press). Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists. ACS Medicinal Chemistry Letters, 8(9), 981–986. https://doi.org/10.1021/acsmedchemlett.7b00315

N-(5-Bromo-3-methoxypyrazin-2-yl)-5-chlorothiophene-2-sulfonamide 1 was identified as a hit in a CCR4 receptor antagonist high throughput screen (HTS) of a sub-set of the AstraZeneca compound bank. As a hit with a lead-like profile, it was an excelle... Read More about Discovery of AZD-2098 and AZD-1678, two potent and bioavailable CCR4 receptor antagonists.

Design and elaboration of a tractable tricyclic scaffold to synthesize druglike inhibitors of dipeptidyl peptidase-4 (DPP-4), antagonists of the C–C Chemokine Receptor Type 5 (CCR5), and highly potent and selective phosphoinositol-3 Kinase δ (PI3Kδ) inhibitors (2017)
Journal Article
Schwehm, C., Kellam, B., Garces, A., Hill, S. J., Kindon, N., Bradshaw, T. D., …Stocks, M. (2017). Design and elaboration of a tractable tricyclic scaffold to synthesize druglike inhibitors of dipeptidyl peptidase-4 (DPP-4), antagonists of the C–C Chemokine Receptor Type 5 (CCR5), and highly potent and selective phosphoinositol-3 Kinase δ (PI3Kδ) inhibitors. Journal of Medicinal Chemistry, 60(4), https://doi.org/10.1021/acs.jmedchem.6b01801

A novel molecular scaffold has been synthesized, and its incorporation into new analogues of biologically active molecules across multiple target classes will be discussed. In these studies, we have shown use of the tricyclic scaffold to synthesize p... Read More about Design and elaboration of a tractable tricyclic scaffold to synthesize druglike inhibitors of dipeptidyl peptidase-4 (DPP-4), antagonists of the C–C Chemokine Receptor Type 5 (CCR5), and highly potent and selective phosphoinositol-3 Kinase δ (PI3Kδ) inhibitors.

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.