Outputs (3)

Molecular recognition of an odorant by the murine trace amine-associated receptor TAAR7f (2024)
Journal Article
Gusach, A., Lee, Y., Khoshgrudi, A. N., Mukhaleva, E., Ma, N., Koers, E. J., Chen, Q., Edwards, P. C., Huang, F., Kim, J., Mancia, F., Veprintsev, D. B., Vaidehi, N., Weyand, S. N., & Tate, C. G. (2024). Molecular recognition of an odorant by the murine trace amine-associated receptor TAAR7f. Nature Communications, 15(1), Article 7555. https://doi.org/10.1038/s41467-024-51793-w

There are two main families of G protein-coupled receptors that detect odours in humans, the odorant receptors (ORs) and the trace amine-associated receptors (TAARs). Their amino acid sequences are distinct, with the TAARs being most similar to the a... Read More about Molecular recognition of an odorant by the murine trace amine-associated receptor TAAR7f.

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., Harwood, C. R., Dijon, N., Holliday, N. D., Sykes, D. A., & 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**.

Combined docking and machine learning identify key molecular determinants of ligand pharmacological activity on β2 adrenoceptor (2022)
Journal Article
Jiménez-Rosés, M., Morgan, B. A., Jimenez Sigstad, M., Tran, T. D. Z., Srivastava, R., Bunsuz, A., Borrega‐Román, L., Hompluem, P., Cullum, S. A., Harwood, C. R., Koers, E. J., Sykes, D. A., Styles, I. B., & Veprintsev, D. B. (2022). Combined docking and machine learning identify key molecular determinants of ligand pharmacological activity on β2 adrenoceptor. Pharmacology Research and Perspectives, 10(5), Article e00994. https://doi.org/10.1002/prp2.994

G protein-coupled receptors (GPCRs) are valuable therapeutic targets for many diseases. A central question of GPCR drug discovery is to understand what determines the agonism or antagonism of ligands that bind them. Ligands exert their action via the... Read More about Combined docking and machine learning identify key molecular determinants of ligand pharmacological activity on β2 adrenoceptor.