Outputs (59)

NanoB2 to monitor interactions of ligands with membrane proteins by combining nanobodies and NanoBRET (2023)
Journal Article
van den Bor, J., Bergkamp, N. D., Anbuhl, S. M., Dekker, F., Comez, D., Perez Almeria, C. V., …Heukers, R. (2023). NanoB2 to monitor interactions of ligands with membrane proteins by combining nanobodies and NanoBRET. Cell Reports Methods, 3(3), Article 100422. https://doi.org/10.1016/j.crmeth.2023.100422

The therapeutic potential of ligands targeting disease-associated membrane proteins is predicted by ligand-receptor binding constants, which can be determined using NanoLuciferase (NanoLuc)-based bioluminescence resonance energy transfer (NanoBRET) m... Read More about NanoB2 to monitor interactions of ligands with membrane proteins by combining nanobodies and NanoBRET.

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.

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.

Fluorescently tagged nanobodies and NanoBRET to study ligand-binding and agonist-induced conformational changes of full-length EGFR expressed in living cells (2022)
Journal Article
Comez, D., Glenn, J., Anbuhl, S. M., Heukers, R., Smit, M. J., Hill, S. J., & Kilpatrick, L. E. (2022). Fluorescently tagged nanobodies and NanoBRET to study ligand-binding and agonist-induced conformational changes of full-length EGFR expressed in living cells. Frontiers in Immunology, 13, Article 1006718. https://doi.org/10.3389/fimmu.2022.1006718

Introduction: The Epidermal Growth Factor Receptor is a member of the Erb receptor tyrosine kinase family. It binds several ligands including EGF, betacellulin (BTC) and TGF-α, controls cellular proliferation and invasion and is overexpressed in vari... Read More about Fluorescently tagged nanobodies and NanoBRET to study ligand-binding and agonist-induced conformational changes of full-length EGFR expressed in living 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.

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.

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.

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.