Outputs (26)

Development and Application of Subtype-Selective Fluorescent Antagonists for the Study of the Human Adenosine A1 Receptor in Living Cells (2021)
Journal Article
Comeo, E., Trinh, P., Nguyen, A. T., Nowell, C. J., Kindon, N. D., Soave, M., Stoddart, L. A., White, J. M., Hill, S. J., Kellam, B., Halls, M. L., May, L. T., & Scammells, P. J. (2021). Development and Application of Subtype-Selective Fluorescent Antagonists for the Study of the Human Adenosine A1 Receptor in Living Cells. Journal of Medicinal Chemistry, 64(10), 6670-6695. https://doi.org/10.1021/acs.jmedchem.0c02067

The adenosine A1 receptor (A1AR) is a G-protein-coupled receptor (GPCR) that provides important therapeutic opportunities for a number of conditions including congestive heart failure, tachycardia, and neuropathic pain. The development of A1AR-select... Read More about Development and Application of Subtype-Selective Fluorescent Antagonists for the Study of the Human Adenosine A1 Receptor in Living Cells.

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.

Subtype-Selective Fluorescent Ligands as Pharmacological Research Tools for the Human Adenosine A2A Receptor (2019)
Journal Article
Comeo, E., Kindon, N. D., Soave, M., Stoddart, L. A., Kilpatrick, L. E., Scammells, P. J., Hill, S. J., & Kellam, B. (2020). Subtype-Selective Fluorescent Ligands as Pharmacological Research Tools for the Human Adenosine A2A Receptor. Journal of Medicinal Chemistry, 63(5), 2656-2672. https://doi.org/10.1021/acs.jmedchem.9b01856

© 2019 American Chemical Society. Among class A G protein-coupled receptors (GPCR), the human adenosine A2A receptor (hA2AAR) remains an attractive drug target. However, translation of A2AAR ligands into the clinic has proved challenging and an impro... Read More about Subtype-Selective Fluorescent Ligands as Pharmacological Research Tools for the Human Adenosine A2A Receptor.

NanoBiT Complementation to Monitor Agonist-Induced Adenosine A1 Receptor Internalization (2019)
Journal Article
Soave, M., Kellam, B., Woolard, J., Briddon, S. J., & Hill, S. J. (2019). NanoBiT Complementation to Monitor Agonist-Induced Adenosine A1 Receptor Internalization. Slas Discovery, https://doi.org/10.1177/2472555219880475

Receptor internalization in response to prolonged agonist treatment is an important regulator of G protein–coupled receptor (GPCR) function. The adenosine A1 receptor (A1AR) is one of the adenosine receptor family of GPCRs, and evidence for its agoni... Read More about NanoBiT Complementation to Monitor Agonist-Induced Adenosine A1 Receptor Internalization.

Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor (2019)
Journal Article
Fyfe, T. J., Kellam, B., Sykes, D. A., Capuano, B., Scammells, P. J., Lane, J. R., Charlton, S. J., & Mistry, S. N. (2019). Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor. Journal of Medicinal Chemistry, 62(21), 9488-9520. https://doi.org/10.1021/acs.jmedchem.9b00864

Haloperidol is a typical antipsychotic drug (APD) associated with an increased risk of extrapyramidal side-effects (EPS) and hyperprolactinemia relative to atypical APDs such as clozapine. Both drugs are dopamine D2 receptor (D2R) antagonists, with c... Read More about Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor.

Modulators of CXCR4 and CXCR7/ACKR3 Function (2019)
Journal Article
Adlere, I., Caspar, B., Arimont, M., Dekkers, S., Visser, K., Stuijt, J., de Graaf, C., Stocks, M., Kellam, B., Briddon, S., Wijtmans, M., de Esch, I., Hill, S., & 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.

Visualising ligand-binding to a GPCR in vivo using nanoBRET (2018)
Journal Article
Carvalheira Alcobia, D., Ziegler, A. I., Kondrashov, A., Comeo, E., Mistry, S., Kellam, B., Chang, A., Woolard, J., Hill, S. J., & Sloan, E. K. (2018). Visualising ligand-binding to a GPCR in vivo using nanoBRET. iScience, 6(8), 280-288. https://doi.org/10.1016/j.isci.2018.08.006

© 2018 The Author(s) The therapeutic action of a drug depends on its ability to engage with its molecular target in vivo. However, current drug discovery strategies quantify drug levels within organs rather than determining the binding of drugs direc... Read More about Visualising ligand-binding to a GPCR in vivo using nanoBRET.

Synthesis and evaluation of the first fluorescent antagonists of the human P2Y2 receptor based on AR-C118925 (2018)
Journal Article
Conroy, S., Kindon, N., Glenn, J., Stoddart, L. A., Lewis, R. J., Hill, S. J., Kellam, B., & Stocks, M. J. (2018). Synthesis and evaluation of the first fluorescent antagonists of the human P2Y2 receptor based on AR-C118925. Journal of Medicinal Chemistry, 61(7), https://doi.org/10.1021/acs.jmedchem.8b00139

The human P2Y2 receptor (hP2Y2R) is a G protein-coupled receptor that shows promise as a therapeutic target for many important conditions including anti-metastatic cancer therapy and more recently for the treatment of idiopathic pulmonary fibrosis. A... Read More about Synthesis and evaluation of the first fluorescent antagonists of the human P2Y2 receptor based on AR-C118925.

Development of novel fluorescent histamine H₁-receptor antagonists to study ligand-binding kinetics in living cells (2018)
Journal Article
Stoddart, L. A., Vernall, A. J., Bouzo-Lorenzo, M., Bosma, R., Kooistra, A. J., de Graaf, C., Vischer, H. F., Leurs, R., Briddon, S. J., Kellam, B., & Hill, S. J. (2018). Development of novel fluorescent histamine H₁-receptor antagonists to study ligand-binding kinetics in living cells. Scientific Reports, 8, Article 1572. https://doi.org/10.1038/s41598-018-19714-2

The histamine H1-receptor (H1R) is an important mediator of allergy and inflammation. H1R antagonists have particular clinical utility in allergic rhinitis and urticaria. Here we have developed six novel fluorescent probes for this receptor that are... Read More about Development of novel fluorescent histamine H₁-receptor antagonists to study ligand-binding kinetics in living cells.

Fluorescently Labeled Morphine Derivatives for Bioimaging Studies (2018)
Journal Article
Lam, R., Gondin, A. B., Canals, M., Kellam, B., Briddon, S. J., Graham, B., & Scammells, P. J. (2018). Fluorescently Labeled Morphine Derivatives for Bioimaging Studies. Journal of Medicinal Chemistry, 61(3), 1316-1329. https://doi.org/10.1021/acs.jmedchem.7b01811

Opioids, like morphine, are the mainstay analgesics for the treatment and control of pain. Despite this, they often exhibit severe side effects that limit dose; patients often become tolerant and dependent on these drugs, which remains a major health... Read More about Fluorescently Labeled Morphine Derivatives for Bioimaging Studies.