All Outputs (4)

Use of NanoBiT and NanoBRET to characterise interleukin-23 receptor dimer formation in living cells (2022)
Journal Article
Lay, C. S., Kilpatrick, L. E., Craggs, P. D., & Hill, S. J. (2023). Use of NanoBiT and NanoBRET to characterise interleukin-23 receptor dimer formation in living cells. British Journal of Pharmacology, 180(11), 1444-1459. https://doi.org/10.1111/bph.16018

Background and Purpose: Interleukin-23 (IL-23) and its receptor are important drug targets for the treatment of auto-inflammatory diseases. IL-23 binds to a receptor complex composed of two single transmembrane spanning proteins IL23R and IL12Rβ1. In... Read More about Use of NanoBiT and NanoBRET to characterise interleukin-23 receptor dimer formation in living cells.

Kinetic analysis of endogenous β2-adrenoceptor-mediated cAMP GloSensorTM responses in HEK293 cells (2022)
Journal Article
Cullum, S. A., Veprintsev, D. B., & Hill, S. J. (2023). Kinetic analysis of endogenous β2-adrenoceptor-mediated cAMP GloSensorTM responses in HEK293 cells. British Journal of Pharmacology, 180(10), 1304-1315. https://doi.org/10.1111/bph.16008

Background and Aim: Standard pharmacological analysis of agonist activity utilises measurements of receptor-mediated responses at a set time-point, or at the peak response level, to characterise ligands. However, the occurrence of non-equilibrium con... Read More about Kinetic analysis of endogenous β2-adrenoceptor-mediated cAMP GloSensorTM responses in HEK293 cells.

Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H1 Receptor (2022)
Journal Article
Kok, Z. Y., Stoddart, L. A., Mistry, S. J., Mocking, T. A., Vischer, H. F., Leurs, R., …Kellam, B. (2022). Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H1 Receptor. Journal of Medicinal Chemistry, 65(12), 8258–8288. https://doi.org/10.1021/acs.jmedchem.2c00125

The histamine H1 receptor (H1R) has recently been implicated in mediating cell proliferation and cancer progression, therefore high affinity H1R-selective fluorescent ligands are desirable tools for further investigation of this behaviour in vitro an... Read More about Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine H1 Receptor.

Community guidelines for GPCR ligand bias: IUPHAR review 32 (2022)
Journal Article
Kolb, P., Kenakin, T., Alexander, S. P. H., Bermudez, M., Bohn, L. M., Breinholt, C. S., …Gloriam, D. E. (2022). Community guidelines for GPCR ligand bias: IUPHAR review 32. British Journal of Pharmacology, 179(14), 3651-3674. https://doi.org/10.1111/bph.15811

GPCRs modulate a plethora of physiological processes and mediate the effects of one-third of FDA-approved drugs. Depending on which ligand activates a receptor, it can engage different intracellular transducers. This ‘biased signalling’ paradigm requ... Read More about Community guidelines for GPCR ligand bias: IUPHAR review 32.