All Outputs (11)

Ligand-Directed Labeling of the Adenosine A1 Receptor in Living Cells (2024)
Journal Article
Comeo, E., Goulding, J., Lin, C.-Y., Groenen, M., Woolard, J., Kindon, N. D., …Kellam, B. (2024). Ligand-Directed Labeling of the Adenosine A1 Receptor in Living Cells. Journal of Medicinal Chemistry, https://doi.org/10.1021/acs.jmedchem.4c00835

The study of protein function and dynamics in their native cellular environment is essential for progressing fundamental science. To overcome the requirement of genetic modification of the protein or the limitations of dissociable fluorescent ligands... Read More about Ligand-Directed Labeling of the Adenosine A1 Receptor in Living Cells.

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.

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.

Use of NanoBiT and NanoBRET to monitor fluorescent VEGF-A binding kinetics to VEGFR2/NRP1 heteromeric complexes in living cells (2021)
Journal Article
Peach, C. J., Kilpatrick, L. E., Woolard, J., & Hill, S. J. (2021). Use of NanoBiT and NanoBRET to monitor fluorescent VEGF-A binding kinetics to VEGFR2/NRP1 heteromeric complexes in living cells. British Journal of Pharmacology, 178(12), 2393-2411. https://doi.org/10.1111/bph.15426

Background and Purpose: VEGF‐A is a key mediator of angiogenesis, primarily signalling via VEGF receptor 2 (VEGFR2). Endothelial cells also express the co‐receptor neuropilin‐1 (NRP1) that potentiates VEGF‐A/VEGFR2 signalling. VEGFR2 and NRP1 had d... Read More about Use of NanoBiT and NanoBRET to monitor fluorescent VEGF-A binding kinetics to VEGFR2/NRP1 heteromeric complexes in living cells.

Ligand-directed covalent labelling of a GPCR with a fluorescent tag in live cells (2020)
Journal Article
Stoddart, L. A., Kindon, N. D., Otun, O., Harwood, C. R., Patera, F., Veprintsev, D. B., …Kellam, B. (2020). Ligand-directed covalent labelling of a GPCR with a fluorescent tag in live cells. Communications Biology, 3(1), Article 722. https://doi.org/10.1038/s42003-020-01451-w

© 2020, The Author(s). To study the localisation of G protein-coupled receptors (GPCR) in their native cellular environment requires their visualisation through fluorescent labelling. To overcome the requirement for genetic modification of the recept... Read More about Ligand-directed covalent labelling of a GPCR with a fluorescent tag in live cells.

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.

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.

Long‐term cardiovascular effects of vandetanib and pazopanib in normotensive rats (2019)
Journal Article
Cooper, S. L., Carter, J. J., March, J., & Woolard, J. (2019). Long‐term cardiovascular effects of vandetanib and pazopanib in normotensive rats. Pharmacology Research and Perspectives, 7(3), Article e00477. https://doi.org/10.1002/prp2.477

Vandetanib and pazopanib are clinically available, multi‐targeted inhibitors of vascular endothelial growth factor (VEGF) and platelet‐derived growth factor (PDGF) receptor tyrosine kinases. Short‐term VEGF receptor inhibition is associated with hype... Read More about Long‐term cardiovascular effects of vandetanib and pazopanib in normotensive rats.

Real-Time Ligand Binding of Fluorescent VEGF-A Isoforms that Discriminate between VEGFR2 and NRP1 in Living Cells (2018)
Journal Article
Peach, C. J., Kilpatrick, L. E., Friedman-Ohana, R., Zimmerman, K., Robers, M. B., Wood, K. V., …Hill, S. J. (2018). Real-Time Ligand Binding of Fluorescent VEGF-A Isoforms that Discriminate between VEGFR2 and NRP1 in Living Cells. Cell Chemical Biology, 25(10), 1208-1218.e5. https://doi.org/10.1016/j.chembiol.2018.06.012

© 2018 The Author(s) Fluorescent VEGF-A isoforms have been evaluated for their ability to discriminate between VEGFR2 and NRP1 in real-time ligand binding studies in live cells using BRET. To enable this, we synthesized single-site (N-terminal cystei... Read More about Real-Time Ligand Binding of Fluorescent VEGF-A Isoforms that Discriminate between VEGFR2 and NRP1 in Living Cells.

Effects of 4 multitargeted receptor tyrosine kinase inhibitors on regional hemodynamics in conscious, freely moving rats (2016)
Journal Article
Carter, J. J., Fretwell, L., & Woolard, J. (2017). Effects of 4 multitargeted receptor tyrosine kinase inhibitors on regional hemodynamics in conscious, freely moving rats. FASEB Journal, 31(3), 1193-1203. https://doi.org/10.1096/fj.201600749r

VEGF inhibitors, including receptor tyrosine kinase inhibitors, are used as adjunct therapies in a number of cancer treatments. An emerging issue with these drugs is that most cause hypertension. To gain insight into the physiological mechanisms invo... Read More about Effects of 4 multitargeted receptor tyrosine kinase inhibitors on regional hemodynamics in conscious, freely moving rats.

Monoclonal anti-β1-adrenergic receptor antibodies activate G protein signaling in the absence of β-arrestin recruitment (2013)
Journal Article
Hutchings, C. J., Cseke, G., Osborne, G., Woolard, J., Zhukov, A., Koglin, M., …Marshall, F. H. (2014). Monoclonal anti-β1-adrenergic receptor antibodies activate G protein signaling in the absence of β-arrestin recruitment. mAbs, 6(1), 246-261. https://doi.org/10.4161/mabs.27226

Thermostabilized G protein-coupled receptors used as antigens for in vivo immunization have resulted in the generation of functional agonistic anti-β1-adrenergic (β1AR) receptor monoclonal antibodies (mAbs). The focus of this study was to examine the... Read More about Monoclonal anti-β1-adrenergic receptor antibodies activate G protein signaling in the absence of β-arrestin recruitment.