All Outputs (4)

The effect of two selective A1-receptor agonists and the bitopic ligand VCP746 on heart rate and regional vascular conductance in conscious rats (2019)
Journal Article
Cooper, S. L., March, J., Sabbatini, A. R., Hill, S. J., Jörg, M., Scammells, P. J., & Woolard, J. (2020). The effect of two selective A1-receptor agonists and the bitopic ligand VCP746 on heart rate and regional vascular conductance in conscious rats. British Journal of Pharmacology, 177(2), 346-359. https://doi.org/10.1111/bph.14870

Background and purpose Adenosine is a local mediator that regulates physiological and pathological processes via activation of four G protein‐coupled receptors (A1, A2A, A2B, A3). We have investigated the effect of two A1‐receptor selective agonists... Read More about The effect of two selective A1-receptor agonists and the bitopic ligand VCP746 on heart rate and regional vascular conductance in conscious rats.

Modulators of CXCR4 and CXCR7/ACKR3 Function (2019)
Journal Article
Adlere, I., Caspar, B., Arimont, M., Dekkers, S., Visser, K., Stuijt, J., …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.

Comparison of the ligand‐binding properties of fluorescent VEGF‐A isoforms to VEGF receptor 2 in living cells and membrane preparations using NanoBRET (2019)
Journal Article
Peach, C. J., Kilpatrick, L. E., Woolard, J., & Hill, S. J. (2019). Comparison of the ligand‐binding properties of fluorescent VEGF‐A isoforms to VEGF receptor 2 in living cells and membrane preparations using NanoBRET. British Journal of Pharmacology, 176(17), 3220-3235. https://doi.org/10.1111/bph.14755

Background and Purpose: Vascular Endothelial Growth Factor A (VEGF-A) is a key mediator of angiogenesis. A striking feature of the binding of a fluorescent analogue of VEGF165a to NanoLuciferase-tagged VEGF Receptor 2 (VEGFR2) in living cells is that... Read More about Comparison of the ligand‐binding properties of fluorescent VEGF‐A isoforms to VEGF receptor 2 in living cells and membrane preparations using NanoBRET.

Binding kinetics of ligands acting at GPCRs (2019)
Journal Article
Sykes, D. A., Stoddart, L. A., Kilpatrick, L. E., & Hill, S. J. (2019). Binding kinetics of ligands acting at GPCRs. Molecular and Cellular Endocrinology, 485, 9-19. https://doi.org/10.1016/j.mce.2019.01.018

The influence of drug-receptor binding kinetics has often been overlooked during the development of new therapeutics that target G protein-coupled receptors (GPCRs). Over the last decade there has been a growing understanding that an in-depth knowled... Read More about Binding kinetics of ligands acting at GPCRs.