Communications Biology (May 2021)

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

DOI
https://doi.org/10.1038/s42003-021-02070-9
Journal volume & issue
Vol. 4, no. 1
pp. 1 – 12

Abstract

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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.