Biased action of the CXCR4-targeting drug plerixafor is essential for its superior hematopoietic stem cell mobilization
2021
Astrid S. Jørgensen | Viktorija Daugvilaite | Katia De Filippo | Christian Berg | Masa Mavri | Tau Benned-Jensen | Goda Juzenaite | Gertrud Hjortø | Sara Rankin | Jon Våbenø | Mette M. Rosenkilde
Jørgensen et al. investigate the effects of the CXCR4 targeting agents, AMD3100 (Plerixafor) and AMD11070, and show that AMD3100, unlike AMD11070, is biased with intrinsic β-arrestin recruitment agonism and full G protein antagonism. They finally propose that this biased action of AMD3100 is central for its superior therapeutic effect on mobilizing stem cells.
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