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Small-Molecule Fluorescent Ligands for the CXCR4 Chemokine Receptor

Dekkers, Sebastian; Caspar, Birgit; Goulding, Joëlle; Kindon, Nicholas D; Kilpatrick, Laura E.; Stoddart, Leigh A; Briddon, Stephen J.; Kellam, Barrie; Hill, Stephen J.; Stocks, Michael J.

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Sebastian Dekkers

Birgit Caspar

Leigh A Stoddart

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Professor of Medicinal Chemistry

Professor of Molecular Pharmacology

Professor of Medicinal Chemistry and Drug Discovery


The C-X-C chemokine receptor type 4, or CXCR4, is a chemokine receptor found to promote cancer progression and metastasis of various cancer cell types. To investigate the pharmacology of this receptor, and to further elucidate its role in cancer, novel chemical tools are a necessity. In the present study, using classic medicinal chemistry approaches, small-molecule-based fluorescent probes were designed and synthesized based on previously reported small-molecule antagonists. Here, we report the development of three distinct chemical classes of fluorescent probes that show specific binding to the CXCR4 receptor in a novel fluorescence-based NanoBRET binding assay (pKD ranging 6.6-7.1). Due to their retained affinity at CXCR4, we furthermore report their use in competition binding experiments and confocal microscopy to investigate the pharmacology and cellular distribution of this receptor.


Dekkers, S., Caspar, B., Goulding, J., Kindon, N. D., Kilpatrick, L. E., Stoddart, L. A., …Stocks, M. J. (2023). Small-Molecule Fluorescent Ligands for the CXCR4 Chemokine Receptor. Journal of Medicinal Chemistry, 66(7), 5208-5222.

Journal Article Type Article
Acceptance Date Mar 9, 2023
Online Publication Date Mar 21, 2023
Publication Date Apr 13, 2023
Deposit Date Mar 10, 2023
Publicly Available Date Mar 22, 2024
Journal Journal of Medicinal Chemistry
Print ISSN 0022-2623
Electronic ISSN 1520-4804
Peer Reviewed Peer Reviewed
Volume 66
Issue 7
Pages 5208-5222
Keywords Antagonists, Fluorescence, Ligands, Mixtures, Receptors
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Additional Information This document is the Accepted Manuscript version of a Published Work that appeared in final form in ACS Journal of Medicinal Chemistry after peer review and technical editing by the publisher. To access the final edited and published work see