Caspar, B., Cocchiara, P., Melet, A., Van Emelen, K., Van der Aa, A., Milligan, G. and Herbeuval, J.-P. (2022) CXCR4 as a novel target in immunology: moving away from typical antagonists. Future Drug Discovery, 4(2), FDD77. (doi: 10.4155/fdd-2022-0007) (PMID:35875591) (PMCID:PMC9298491)
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Abstract
CXCR4 has been a target of interest in drug discovery for numerous years. However, so far, most if not all studies focused on finding antagonists of CXCR4 function. Recent studies demonstrate that targeting a minor allosteric pocket of CXCR4 induces an immunomodulating effect in immune cells expressing CXCR4, connected to the TLR pathway. Compounds binding in this minor pocket seem to be functionally selective with inverse agonistic properties in selected GPCR signaling pathways (Gi activation), but additional signaling pathways are likely to be involved in the immunomodulating effects. In depth research into these CXCR4-targeted immunomodulators could lead to novel treatment options for (auto)-immune diseases.
Item Type: | Articles |
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Additional Information: | P Cocchiara and G Milligan are supported by the EU (H2020-MSCA Program, Grant Agreement 860229-ONCORNET 2.0). The group of J-P Herbeuval is supported by the Agence nationale de Recherche (grant number ANR-21-CE15-0048 X4Inflam). |
Status: | Published |
Refereed: | Yes |
Glasgow Author(s) Enlighten ID: | Milligan, Professor Graeme |
Authors: | Caspar, B., Cocchiara, P., Melet, A., Van Emelen, K., Van der Aa, A., Milligan, G., and Herbeuval, J.-P. |
College/School: | College of Medical Veterinary and Life Sciences > School of Molecular Biosciences |
Journal Name: | Future Drug Discovery |
Publisher: | Newlands Press |
ISSN: | 2631-3316 |
ISSN (Online): | 2631-3316 |
Published Online: | 19 July 2022 |
Copyright Holders: | Copyright © 2022 Caspar, Birgit |
First Published: | First published in Future Drug Discovery 4(2):FDD77 |
Publisher Policy: | Reproduced under a Creative Commons Licence |
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