All Outputs (5)

NanoBiT Complementation to Monitor Agonist-Induced Adenosine A1 Receptor Internalization (2019)
Journal Article
Soave, M., Kellam, B., Woolard, J., Briddon, S. J., & Hill, S. J. (2019). NanoBiT Complementation to Monitor Agonist-Induced Adenosine A1 Receptor Internalization. Slas Discovery, https://doi.org/10.1177/2472555219880475

Receptor internalization in response to prolonged agonist treatment is an important regulator of G protein–coupled receptor (GPCR) function. The adenosine A1 receptor (A1AR) is one of the adenosine receptor family of GPCRs, and evidence for its agoni... Read More about NanoBiT Complementation to Monitor Agonist-Induced Adenosine A1 Receptor Internalization.

Modulators of CXCR4 and CXCR7/ACKR3 Function (2019)
Journal Article
Adlere, I., Caspar, B., Arimont, M., Dekkers, S., Visser, K., Stuijt, J., de Graaf, C., Stocks, M., Kellam, B., Briddon, S., Wijtmans, M., de Esch, I., Hill, S., & Leurs, R. (2019). Modulators of CXCR4 and CXCR7/ACKR3 Function. Molecular Pharmacology, 96(6), 737-752. https://doi.org/10.1124/mol.119.117663

Copyright © 2019 by The Author(s). The two G protein-coupled receptors (GPCRs) C-X-C chemokine receptor type 4 (CXCR4) and atypical chemokine receptor 3 (ACKR3) are part of the class A chemokine GPCR family and represent important drug targets for hu... Read More about Modulators of CXCR4 and CXCR7/ACKR3 Function.

Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor (2019)
Journal Article
Bosma, R., Stoddart, L. A., Georgi, V., Bouzo-Lorenzo, M., Bushby, N., Inkoom, L., Waring, M. J., Briddon, S. J., Vischer, H. F., Sheppard, R. J., Fernández-Montalván, A., Hill, S. J., & Leurs, R. (2019). Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor. Scientific Reports, 9, Article 7906. https://doi.org/10.1038/s41598-019-44025-5

© 2019, The Author(s). Drug-target binding kinetics are suggested to be important parameters for the prediction of in vivo drug-efficacy. For G protein-coupled receptors (GPCRs), the binding kinetics of ligands are typically determined using associat... Read More about Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor.

GRK mediates μ-opioid receptor plasma membrane reorganization (2019)
Journal Article
Gondin, A. B., Halls, M. L., Canals, M., & Briddon, S. J. (2019). GRK mediates μ-opioid receptor plasma membrane reorganization. Frontiers in Molecular Neuroscience, 12, https://doi.org/10.3389/fnmol.2019.00104

Differential regulation of the μ-opioid receptor (MOP) has been linked to the development of opioid tolerance and dependence which both limit the clinical use of opioid analgesics. At a cellular level, MOP regulation occurs via receptor phosphorylati... Read More about GRK mediates μ-opioid receptor plasma membrane reorganization.

A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A3 receptor (2019)
Journal Article
Bouzo-Lorenzo, M., Stoddart, L. A., Xia, L., Jerzman, A. P., Heitman, L. H., Briddon, S. J., & Hill, S. J. (2019). A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A3 receptor. Purinergic Signalling, 15(2), 139–153. https://doi.org/10.1007/s11302-019-09650-9

There is a growing interest in understanding the binding kinetics of compounds that bind to G proteincoupled receptors prior to progressing a lead compound into clinical trials. The widely expressed adenosine A3 receptor (A3AR) has been implicated in... Read More about A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A3 receptor.