Characterisation of endogenous A2A and A2B receptor-mediated cyclic AMP responses in HEK 293 cells using the GloSensor™ biosensor: evidence for an allosteric mechanism of action for the A2B-selective antagonist PSB 603

Goulding, Joelle; May, Lauren T.; Hill, Stephen J.

doi:10.1016/j.bcp.2017.10.013

All Outputs (9)

A novel and selective fluorescent ligand for the study of adenosine A2B receptors (2024)
Journal Article
Patera, F., Mistry, S. J., Kindon, N. D., Comeo, E., Gouding, J., Kellam, B., Kilpatrick, L. E., Franks, H., & Hill, S. J. (2024). A novel and selective fluorescent ligand for the study of adenosine A2B receptors. Pharmacology Research and Perspectives, 12(4), Article e1223. https://doi.org/10.1002/prp2.1223

Fluorescent ligands have proved to be powerful tools in the study of G protein-coupled receptors in living cells. Here we have characterised a new fluorescent ligand PSB603-BY630 that has high selectivity for the human adenosine A2B receptor (A2BR).... Read More about A novel and selective fluorescent ligand for the study of adenosine A2B receptors.

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.

Plasma membrane preassociation drives β-arrestin coupling to receptors and activation (2023)
Journal Article
Grimes, J., Koszegi, Z., Lanoiselée, Y., Miljus, T., O’Brien, S. L., Stepniewski, T. M., …Calebiro, D. (2023). Plasma membrane preassociation drives β-arrestin coupling to receptors and activation. Cell, 186(10), 2238-2255. https://doi.org/10.1016/j.cell.2023.04.018

β-arrestin plays a key role in G protein-coupled receptor (GPCR) signaling and desensitization. Despite recent structural advances, the mechanisms that govern receptor-β-arrestin interactions at the plasma membrane of living cells remain elusive. Her... Read More about Plasma membrane preassociation drives β-arrestin coupling to receptors and activation.

Probing the binding of interleukin-23 to individual receptor components and the IL-23 heteromeric receptor complex in living cells using NanoBRET (2021)
Journal Article
Lay, C. S., Bridges, A., Goulding, J., Briddon, S. J., Soloviev, Z., Craggs, P. D., & Hill, S. J. (2022). Probing the binding of interleukin-23 to individual receptor components and the IL-23 heteromeric receptor complex in living cells using NanoBRET. Cell Chemical Biology, 29(1), 19-29.e6. https://doi.org/10.1016/j.chembiol.2021.05.002

Interleukin-23 (IL-23) is a pro-inflammatory cytokine involved in the host defence against pathogens, but also implicated in the development of several autoimmune disorders. The IL- 23 receptor has become a key target for drug discovery but the exact... Read More about Probing the binding of interleukin-23 to individual receptor components and the IL-23 heteromeric receptor complex in living cells using NanoBRET.

Subtype selective fluorescent ligands based on ICI 118,551 to study the human β2‐adrenoceptor in CRISPR/Cas9 genome‐edited HEK293T cells at low expression levels (2021)
Journal Article
Kellam, B., White, C. W., Goulding, J., Mistry, S. J., Soave, M., Woolard, J., …Hill, S. J. (2021). Subtype selective fluorescent ligands based on ICI 118,551 to study the human β2‐adrenoceptor in CRISPR/Cas9 genome‐edited HEK293T cells at low expression levels. Pharmacology Research and Perspectives, 9(3), Article e00779. https://doi.org/10.1002/prp2.779

Fluorescent ligand technologies have proved to be powerful tools to improve our understanding of ligand-receptor interactions. Here we have characterized a small focused library of nine fluorescent ligands based on the highly selective β2-adrenocepto... Read More about Subtype selective fluorescent ligands based on ICI 118,551 to study the human β2‐adrenoceptor in CRISPR/Cas9 genome‐edited HEK293T cells at low expression levels.

Detection of genome-edited and endogenously expressed G protein-coupled receptors (2021)
Journal Article
Soave, M., Stoddart, L. A., White, C. W., Kilpatrick, L. E., Goulding, J., Briddon, S. J., & Hill, S. J. (2021). Detection of genome-edited and endogenously expressed G protein-coupled receptors. FEBS Journal, 288(8), 2585-2601. https://doi.org/10.1111/febs.15729

© 2021 The Authors. The FEBS Journal published by John Wiley & Sons Ltd on behalf of Federation of European Biochemical Societies. G protein-coupled receptors (GPCRs) are the largest family of membrane receptors and major targets for FDA-approved d... Read More about Detection of genome-edited and endogenously expressed G protein-coupled receptors.

CRISPR/Cas9-mediated generation and analysis of N terminus polymorphic models of β2AR in isogenic hPSC-derived cardiomyocytes (2020)
Journal Article
Kondrashov, A., Mohd Yusof, N. A., Hasan, A., Goulding, J., Kodagoda, T., Hoang, D. M., …Denning, C. (2021). CRISPR/Cas9-mediated generation and analysis of N terminus polymorphic models of β2AR in isogenic hPSC-derived cardiomyocytes. Molecular Therapy - Methods and Clinical Development, 20, 39-53. https://doi.org/10.1016/j.omtm.2020.10.019

© 2020 During normal- and patho-physiological situations, the behavior of the beta2-adrenoreceptor (β2AR) is influenced by polymorphic variants. The functional impact of such polymorphisms has been suggested from data derived from genetic association... Read More about CRISPR/Cas9-mediated generation and analysis of N terminus polymorphic models of β2AR in isogenic hPSC-derived cardiomyocytes.

The tetraspanin Tspan15 is an essential subunit of an ADAM10 scissor complex (2020)
Journal Article
Koo, C. Z., Harrison, N., Noy, P. J., Szyroka, J., Matthews, A. L., Hsia, H. E., …Tomlinson, M. G. (2020). The tetraspanin Tspan15 is an essential subunit of an ADAM10 scissor complex. Journal of Biological Chemistry, 295(36), 12822-12839. https://doi.org/10.1074/jbc.RA120.012601

© 2020 Koo et al. A disintegrin and metalloprotease 10 (ADAM10) is a transmembrane protein essential for embryonic development, and its dysregulation underlies disorders such as cancer, Alzheimer's disease, and inflammation. ADAM10 is a "molecular sc... Read More about The tetraspanin Tspan15 is an essential subunit of an ADAM10 scissor complex.

Characterisation of endogenous A2A and A2B receptor-mediated cyclic AMP responses in HEK 293 cells using the GloSensor™ biosensor: evidence for an allosteric mechanism of action for the A2B-selective antagonist PSB 603 (2017)
Journal Article
Goulding, J., May, L. T., & Hill, S. J. (2018). Characterisation of endogenous A2A and A2B receptor-mediated cyclic AMP responses in HEK 293 cells using the GloSensor™ biosensor: evidence for an allosteric mechanism of action for the A2B-selective antagonist PSB 603. Biochemical Pharmacology, 147, https://doi.org/10.1016/j.bcp.2017.10.013

Endogenous adenosine A2B receptors (A2BAR) mediate cAMP accumulation in HEK 293 cells. Here we have used a biosensor to investigate the mechanism of action of the A2BAR antagonist PSB 603 in HEK 293 cells. The A2A agonist CGS 21680 elicited a small r... Read More about Characterisation of endogenous A2A and A2B receptor-mediated cyclic AMP responses in HEK 293 cells using the GloSensor™ biosensor: evidence for an allosteric mechanism of action for the A2B-selective antagonist PSB 603.