Modulators of CXCR4 and CXCR7/ACKR3 Function

Adlere, Ilze; Caspar, Birgit; Arimont, Marta; Dekkers, Sebastian; Visser, Kirsten; Stuijt, Jeffrey; de Graaf, Chris; Stocks, Michael; Kellam, Barrie; Briddon, Stephen; Wijtmans, Maikel; de Esch, Iwan; Hill, Stephen; Leurs, Rob

doi:10.1124/mol.119.117663

All Outputs (3)

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., …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.

Modulators of CXCR4 and CXCR7/ACKR3 Function (2019)
Journal Article
Adlere, I., Caspar, B., Arimont, M., Dekkers, S., Visser, K., Stuijt, J., …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.