All Outputs (4)

Dually Labeled Neurotensin NTS1R Ligands for Probing Radiochemical and Fluorescence-Based Binding Assays (2024)
Journal Article
Ertl, F. J., Kopanchuk, S., Dijon, N. C., Veikšina, S., Tahk, M.-J., Laasfeld, T., Schettler, F., Gattor, A. O., Hübner, H., Archipowa, N., Köckenberger, J., Heinrich, M. R., Gmeiner, P., Kutta, R. J., Holliday, N. D., Rinken, A., & Keller, M. (2024). Dually Labeled Neurotensin NTS1R Ligands for Probing Radiochemical and Fluorescence-Based Binding Assays. Journal of Medicinal Chemistry, https://doi.org/10.1021/acs.jmedchem.4c01470

The determination of ligand-receptor binding affinities plays a key role in the development process of pharmaceuticals. While the classical radiochemical binding assay uses radioligands, fluorescence-based binding assays require fluorescent probes. U... Read More about Dually Labeled Neurotensin NTS1R Ligands for Probing Radiochemical and Fluorescence-Based Binding Assays.

High-throughput kinetics in drug discovery (2024)
Journal Article
Pinto, M. F., Sirina, J., Holliday, N. D., & McWhirter, C. L. (2024). High-throughput kinetics in drug discovery. Slas Discovery, 29(5), Article 100170. https://doi.org/10.1016/j.slasd.2024.100170

The importance of a drug's kinetic profile and interplay of structure-kinetic activity with PK/PD has long been appreciated in drug discovery. However, technical challenges have often limited detailed kinetic characterization of compounds to the latt... Read More about High-throughput kinetics in drug discovery.

The novel adrenergic agonist ATR-127 targets skeletal muscle and brown adipose tissue to tackle diabesity and steatohepatitis (2024)
Journal Article
Talamonti, E., Davegardh, J., Kalinovich, A., van Beek, S. M. M., Dehvari, N., Halleskog, C., Bokhari, H. M., Hutchinson, D. S., Ham, S., Humphrys, L. J., Dijon, N. C., Motso, A., Sandstrom, A., Zacharewicz, E., Mutule, I., Suna, E., Spura, J., Ditrychova, K., Stoddart, L. A., Holliday, N. D., …Bengtsson, T. (2024). The novel adrenergic agonist ATR-127 targets skeletal muscle and brown adipose tissue to tackle diabesity and steatohepatitis. Molecular Metabolism, 85, Article 101931. https://doi.org/10.1016/j.molmet.2024.101931

Objective
Simultaneous activation of β2- and β3-adrenoceptors (ARs) improves whole-body metabolism via beneficial effects in skeletal muscle and brown adipose tissue (BAT). Nevertheless, high-efficacy agonists simultaneously targeting these receptor... Read More about The novel adrenergic agonist ATR-127 targets skeletal muscle and brown adipose tissue to tackle diabesity and steatohepatitis.

Role of G protein‐coupled receptor kinases (GRKs) in β2‐adrenoceptor‐mediated glucose uptake (2024)
Journal Article
Ham, S., Mukaida, S., Sato, M., Keov, P., Bengtsson, T., Furness, S., Holliday, N. D., Evans, B. A., Summers, R. J., & Hutchinson, D. S. (2024). Role of G protein‐coupled receptor kinases (GRKs) in β2‐adrenoceptor‐mediated glucose uptake. Pharmacology Research and Perspectives, 12(1), Article e1176. https://doi.org/10.1002/prp2.1176

Truncation of the C‐terminal tail of the β2‐AR, transfection of βARKct or over‐expression of a kinase‐dead GRK mutant reduces isoprenaline‐stimulated glucose uptake, indicating that GRK is important for this response. We explored whether phosphorylat... Read More about Role of G protein‐coupled receptor kinases (GRKs) in β2‐adrenoceptor‐mediated glucose uptake.