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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., …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.

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.

Development of novel fluorescent histamine H?-receptor antagonists to study ligand-binding kinetics in living cells (2018)
Journal Article
Stoddart, L. A., Vernall, A. J., Bouzo-Lorenzo, M., Bosma, R., Kooistra, A. J., de Graaf, C., …Hill, S. J. (2018). Development of novel fluorescent histamine H₁-receptor antagonists to study ligand-binding kinetics in living cells. Scientific Reports, 8, Article 1572. https://doi.org/10.1038/s41598-018-19714-2

The histamine H1-receptor (H1R) is an important mediator of allergy and inflammation. H1R antagonists have particular clinical utility in allergic rhinitis and urticaria. Here we have developed six novel fluorescent probes for this receptor that are... Read More about Development of novel fluorescent histamine H?-receptor antagonists to study ligand-binding kinetics in living cells.