All Outputs (2)

ThermoBRET: A Ligand-Engagement Nanoscale Thermostability Assay Applied to GPCRs** (2023)
Journal Article
Hoare, B. L., Tippett, D. N., Kaur, A., Cullum, S. A., Miljuš, T., Koers, E. J., …Veprintsev, D. B. (2024). ThermoBRET: A Ligand-Engagement Nanoscale Thermostability Assay Applied to GPCRs**. ChemBioChem, 25(2), Article e202300459. https://doi.org/10.1002/cbic.202300459

Measurements of membrane protein thermostability reflect ligand binding. Current thermostability assays often require protein purification or rely on pre-existing radiolabelled or fluorescent ligands, limiting their application to established targets... Read More about ThermoBRET: A Ligand-Engagement Nanoscale Thermostability Assay Applied to GPCRs**.

Design, Synthesis, and Application of Fluorescent Ligands Targeting the Intracellular Allosteric Binding Site of the CXC Chemokine Receptor 2 (2023)
Journal Article
Casella, B. M., Farmer, J. P., Nesheva, D. N., Williams, H. E., Charlton, S. J., Holliday, N. D., …Mistry, S. N. (2023). Design, Synthesis, and Application of Fluorescent Ligands Targeting the Intracellular Allosteric Binding Site of the CXC Chemokine Receptor 2. Journal of Medicinal Chemistry, https://doi.org/10.1021/acs.jmedchem.3c00849

The inhibition of CXC chemokine receptor 2 (CXCR2), a key inflammatory mediator, is a potential strategy in the treatment of several pulmonary diseases and cancers. The complexity of endogenous chemokine interaction with the orthosteric binding site... Read More about Design, Synthesis, and Application of Fluorescent Ligands Targeting the Intracellular Allosteric Binding Site of the CXC Chemokine Receptor 2.