Outputs (34)

Key phosphorylation sites for robust β-arrestin2 binding at the MOR revisited (2024)
Journal Article
Underwood, O., Fritzwanker, S., Glenn, J., Blum, N. K., Batista-Gondin, A., Drube, J., Hoffmann, C., Briddon, S. J., Schulz, S., & Canals, M. (2024). Key phosphorylation sites for robust β-arrestin2 binding at the MOR revisited. Communications Biology, 7, Article 933. https://doi.org/10.1038/s42003-024-06571-1

Desensitisation of the mu-opioid receptor (MOR) is proposed to underlie the initiation of opioid analgesic tolerance and previous work has shown that agonist-induced phosphorylation of the MOR C-tail contributes to this desensitisation. Moreover, pho... Read More about Key phosphorylation sites for robust β-arrestin2 binding at the MOR revisited.

Ligand-Directed Labeling of the Adenosine A1 Receptor in Living Cells (2024)
Journal Article
Comeo, E., Goulding, J., Lin, C.-Y., Groenen, M., Woolard, J., Kindon, N. D., Harwood, C. R., Platt, S., Briddon, S. J., Kilpatrick, L. E., Scammells, P. J., Hill, S. J., & Kellam, B. (2024). Ligand-Directed Labeling of the Adenosine A1 Receptor in Living Cells. Journal of Medicinal Chemistry, 67(14), 12099–12117. https://doi.org/10.1021/acs.jmedchem.4c00835

The study of protein function and dynamics in their native cellular environment is essential for progressing fundamental science. To overcome the requirement of genetic modification of the protein or the limitations of dissociable fluorescent ligands... Read More about Ligand-Directed Labeling of the Adenosine A1 Receptor in Living Cells.

A high-affinity, cis-on photoswitchable beta blocker to optically control β2-adrenergic receptors in vitro and in vivo (2024)
Journal Article
Shi, S., Zheng, Y., Goulding, J., Marri, S., Lucarini, L., Konecny, B., Sgambellone, S., Villano, S., Bosma, R., Wijtmans, M., Briddon, S. J., Zarzycka, B. A., Vischer, H. F., & Leurs, R. (2024). A high-affinity, cis-on photoswitchable beta blocker to optically control β2-adrenergic receptors in vitro and in vivo. Biochemical Pharmacology, 226, Article 116396. https://doi.org/10.1016/j.bcp.2024.116396

This study introduces (S)-Opto-prop-2, a second-generation photoswitchable ligand designed for precise modulation of β -adrenoceptor (β AR). Synthesised by incorporating an azobenzene moiety with propranolol, (S)-Opto-prop-2 exhibited a high PSS (ph... Read More about A high-affinity, cis-on photoswitchable beta blocker to optically control β2-adrenergic receptors in vitro and in vivo.

Small Molecule Fluorescent Ligands for the Atypical Chemokine Receptor 3 (ACKR3) (2023)
Journal Article
Dekkers, S., Comez, D., Karsai, N., Arimont-Segura, M., Canals, M., Caspar, B., de Graaf, C., Kilpatrick, L. E., Leurs, R., Kellam, B., Hill, S. J., Briddon, S. J., & Stocks, M. J. (2024). Small Molecule Fluorescent Ligands for the Atypical Chemokine Receptor 3 (ACKR3). ACS Medicinal Chemistry Letters, 15(1), 143–148. https://doi.org/10.1021/acsmedchemlett.3c00469

The atypical chemokine receptor 3 (ACKR3) is a receptor that induces cancer progression and metastasis in multiple cell types. Therefore, new chemical tools are required to study the role of ACKR3 in cancer and other diseases. In this study, fluoresc... Read More about Small Molecule Fluorescent Ligands for the Atypical Chemokine Receptor 3 (ACKR3).

A time-resolved Förster resonance energy transfer assay to investigate inhibitor binding to ABCG2 (2023)
Preprint / Working Paper
Mitchell-White, J. I., Briggs, D. A., Mistry, S. J., Mbiwan, H. A., Kellam, B., Holliday, N. D., Briddon, S. J., & Kerr, I. D. A time-resolved Förster resonance energy transfer assay to investigate inhibitor binding to ABCG2

The human ATP-binding cassette (ABC) transporter, ABCG2 is responsible for multidrug resistance in some tumours. Detailed knowledge of its activity is crucial for understanding drug transport and resistance in cancer, and has implications for wider p... Read More about A time-resolved Förster resonance energy transfer assay to investigate inhibitor binding to ABCG2.

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., Briddon, S. J., Kellam, B., Hill, S. J., & 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.

Bitter taste sensitivity in domestic dogs (Canis familiaris) and its relevance to bitter deterrents of ingestion (2022)
Journal Article
Gibbs, M., Winnig, M., Riva, I., Dunlop, N., Waller, D., Klebansky, B., Logan, D. W., Briddon, S. J., Holliday, N. D., & McGrane, S. J. (2022). Bitter taste sensitivity in domestic dogs (Canis familiaris) and its relevance to bitter deterrents of ingestion. PLoS ONE, 17(11), Article e0277607. https://doi.org/10.1371/journal.pone.0277607

As the most favoured animal companion of humans, dogs occupy a unique place in society. Understanding the senses of the dog can bring benefits to both the dogs themselves and their owners. In the case of bitter taste, research may provide useful info... Read More about Bitter taste sensitivity in domestic dogs (Canis familiaris) and its relevance to bitter deterrents of ingestion.

Acylation of the incretin peptide exendin-4 directly impacts glucagon-like peptide-1 receptor signaling and traffickings (2021)
Journal Article
Lucey, M., Ashik, T., Marzook, A., Wang, Y., Goulding, J., Oishi, A., Broichhagen, J., Hodson, D. J., Minnion, J., Elani, Y., Jockers, R., Briddon, S. J., Bloom, S. R., Tomas, A., & Jones, B. (2021). Acylation of the incretin peptide exendin-4 directly impacts glucagon-like peptide-1 receptor signaling and traffickings. Molecular Pharmacology, 100(4), 319-334. https://doi.org/10.1124/molpharm.121.000270

The glucagon-like peptide-1 receptor (GLP-1R) is a class B G protein- coupled receptor and mainstay therapeutic target for the treatment of type 2 diabetes and obesity. Recent reports have highlighted how biased agonism at the GLP-1R affects sustaine... Read More about Acylation of the incretin peptide exendin-4 directly impacts glucagon-like peptide-1 receptor signaling and traffickings.

Probing the binding of interleukin-23 to individual receptor components and the IL-23 heteromeric receptor complex in living cells using NanoBRET (2021)
Journal Article
Lay, C. S., Bridges, A., Goulding, J., Briddon, S. J., Soloviev, Z., Craggs, P. D., & Hill, S. J. (2022). Probing the binding of interleukin-23 to individual receptor components and the IL-23 heteromeric receptor complex in living cells using NanoBRET. Cell Chemical Biology, 29(1), 19-29.e6. https://doi.org/10.1016/j.chembiol.2021.05.002

Interleukin-23 (IL-23) is a pro-inflammatory cytokine involved in the host defense against pathogens but is also implicated in the development of several autoimmune disorders. The IL-23 receptor has become a key target for drug discovery, but the exa... Read More about Probing the binding of interleukin-23 to individual receptor components and the IL-23 heteromeric receptor complex in living cells using NanoBRET.

Analysis of sequence divergence in mammalian abcgs predicts a structural network of residues that underlies functional divergence (2021)
Journal Article
Mitchell-White, J. I., Stockner, T., Holliday, N., Briddon, S. J., & Kerr, I. D. (2021). Analysis of sequence divergence in mammalian abcgs predicts a structural network of residues that underlies functional divergence. International Journal of Molecular Sciences, 22(6), 1-16. https://doi.org/10.3390/ijms22063012

© 2021 by the authors. Licensee MDPI, Basel, Switzerland. The five members of the mammalian G subfamily of ATP-binding cassette transporters differ greatly in their substrate specificity. Four members of the subfamily are important in lipid transport... Read More about Analysis of sequence divergence in mammalian abcgs predicts a structural network of residues that underlies functional divergence.