Biased action of the CXCR4-targeting drug plerixafor is essential for its superior hematopoietic stem cell mobilization

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

Biased action of the CXCR4-targeting drug plerixafor is essential for its superior hematopoietic stem cell mobilization

2021

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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