Outputs (24)

Mechano-sensitivity of β2-adrenoceptors enhances constitutive activation of cAMP generation that is inhibited by inverse agonists (2024)
Journal Article
Cullum, S. A., Platt, S., Dale, N., Isaac, O. C., Wragg, E. S., Soave, M., …Hill, S. J. (2024). Mechano-sensitivity of β2-adrenoceptors enhances constitutive activation of cAMP generation that is inhibited by inverse agonists. Communications Biology, 7(1), Article 417. https://doi.org/10.1038/s42003-024-06128-2

The concept of agonist-independent signalling that can be attenuated by inverse agonists is a fundamental element of the cubic ternary complex model of G protein-coupled receptor (GPCR) activation. This model shows how a GPCR can exist in two conform... Read More about Mechano-sensitivity of β2-adrenoceptors enhances constitutive activation of cAMP generation that is inhibited by inverse agonists.

Role of endothelin ETA receptors in the hypertension induced by the VEGFR-2 kinase inhibitors axitinib and lenvatinib in conscious freely-moving rats (2023)
Journal Article
Pannucci, P., Van Daele, M., Cooper, S. L., Wragg, E. S., March, J., Groenen, M., …Woolard, J. (2023). Role of endothelin ETA receptors in the hypertension induced by the VEGFR-2 kinase inhibitors axitinib and lenvatinib in conscious freely-moving rats. Biochemical Pharmacology, Article 116007. https://doi.org/10.1016/j.bcp.2023.116007

Receptor tyrosine kinase inhibitors (RTKIs) suppress tumour growth by targeting vascular endothelial growth factor receptor 2 (VEGFR-2) which is an important mediator of angiogenesis. Here, we demonstrate that two potent RTKIs, axitinib and lenvatini... Read More about Role of endothelin ETA receptors in the hypertension induced by the VEGFR-2 kinase inhibitors axitinib and lenvatinib in conscious freely-moving rats.

Characterisation of tyrosine kinase inhibitor-receptor interactions at VEGFR2 using sunitinib-red and nanoBRET (2023)
Journal Article
Van Daele, M., Kilpatrick, L. E., Woolard, J., & Hill, S. J. (2023). Characterisation of tyrosine kinase inhibitor-receptor interactions at VEGFR2 using sunitinib-red and nanoBRET. Biochemical Pharmacology, 214, Article 115672. https://doi.org/10.1016/j.bcp.2023.115672

Vascular endothelial growth factor (VEGF) is an important mediator of angiogenesis, proliferation and migration of vascular endothelial cells. It is well known that cardiovascular safety liability for a wide range of small molecule tyrosine kinase in... Read More about Characterisation of tyrosine kinase inhibitor-receptor interactions at VEGFR2 using sunitinib-red and nanoBRET.

Probing expression of E-selectin using CRISPR-Cas9-mediated tagging with HiBiT in human endothelial cells (2023)
Journal Article
Ogrodzinski, L., Platt, S., Goulding, J., Alexander, C., Farr, T. D., Woolard, J., …Kilpatrick, L. E. (2023). Probing expression of E-selectin using CRISPR-Cas9-mediated tagging with HiBiT in human endothelial cells. iScience, 26(7), Article 107232. https://doi.org/10.1016/j.isci.2023.107232

E-selectin is expressed on endothelial cells in response to inflammatory cytokines and mediates leukocyte rolling and extravasation. However, studies have been hampered by lack of experimental approaches to monitor expression in real time in living c... Read More about Probing expression of E-selectin using CRISPR-Cas9-mediated tagging with HiBiT in human endothelial cells.

COVID-19-Induced Myocarditis: Pathophysiological Roles of ACE2 and Toll-like Receptors (2023)
Journal Article
Pannucci, P., Jefferson, S. R., Hampshire, J., Cooper, S. L., Hill, S. J., & Woolard, J. (2023). COVID-19-Induced Myocarditis: Pathophysiological Roles of ACE2 and Toll-like Receptors. International Journal of Molecular Sciences, 24(6), Article 5374. https://doi.org/10.3390/ijms24065374

The clinical manifestations of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection responsible for coronavirus disease 2019 (COVID-19) commonly include dyspnoea and fatigue, and they primarily involve the lungs. However, extra-... Read More about COVID-19-Induced Myocarditis: Pathophysiological Roles of ACE2 and Toll-like Receptors.

Involvement of β-adrenoceptors in the cardiovascular responses induced by selective adenosine A2A and A2B receptor agonists (2022)
Journal Article
Wragg, E. S., Pannucci, P., Hill, S. J., Woolard, J., & Cooper, S. L. (2022). Involvement of β-adrenoceptors in the cardiovascular responses induced by selective adenosine A2A and A2B receptor agonists. Pharmacology Research and Perspectives, 10(3), Article e00975. https://doi.org/10.1002/prp2.975

A2A and A2B adenosine receptors produce regionally selective regulation of vascular tone and elicit differing effects on mean arterial pressure (MAP), whilst inducing tachycardia. The tachycardia induced by the stimulation of A2A or A2B receptors has... Read More about Involvement of β-adrenoceptors in the cardiovascular responses induced by selective adenosine A2A and A2B receptor agonists.

Regionally selective cardiovascular responses to adenosine A2A and A2B receptor activation (2022)
Journal Article
Cooper, S. L., Wragg, E. S., Pannucci, P., Soave, M., Hill, S. J., & Woolard, J. (2022). Regionally selective cardiovascular responses to adenosine A2A and A2B receptor activation. FASEB Journal, 36(4), Article e22214. https://doi.org/10.1096/fj.202101945R

Adenosine is a local mediator that regulates changes in the cardiovascular system via activation of four G protein-coupled receptors (A1, A2A, A2B, A3). Here, we have investigated the effect of A2A and A2B-selective agonists on vasodilatation in thre... Read More about Regionally selective cardiovascular responses to adenosine A2A and A2B receptor activation.

Role of the renin–angiotensin–aldosterone and kinin–kallikrein systems in the cardiovascular complications of COVID-19 and long COVID (2021)
Journal Article
Cooper, S. L., Boyle, E., Jefferson, S. R., Heslop, C. R. A., Mohan, P., Mohanraj, G. G. J., …Woolard, J. (2021). Role of the renin–angiotensin–aldosterone and kinin–kallikrein systems in the cardiovascular complications of COVID-19 and long COVID. International Journal of Molecular Sciences, 22(15), Article 8255. https://doi.org/10.3390/ijms22158255

Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) is the virus responsible for the COVID-19 pandemic. Patients may present as asymptomatic or demonstrate mild to severe and life-threatening symptoms. Although COVID-19 has a respiratory foc... Read More about Role of the renin–angiotensin–aldosterone and kinin–kallikrein systems in the cardiovascular complications of COVID-19 and long COVID.

Monitoring Allosteric Interactions with CXCR4 Using NanoBiT Conjugated Nanobodies (2020)
Journal Article
Soave, M., Heukers, R., Kellam, B., Woolard, J., Smit, M. J., Briddon, S. J., & Hill, S. J. (2020). Monitoring Allosteric Interactions with CXCR4 Using NanoBiT Conjugated Nanobodies. Cell Chemical Biology, 27, 1-12. https://doi.org/10.1016/j.chembiol.2020.06.006

© 2020 The Authors Camelid single-domain antibody fragments (nanobodies) offer the specificity of an antibody in a single 15-kDa immunoglobulin domain. Their small size allows for easy genetic manipulation of the nanobody sequence to incorporate prot... Read More about Monitoring Allosteric Interactions with CXCR4 Using NanoBiT Conjugated Nanobodies.

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.