AMD3100 Is a CXCR7 Ligand with Allosteric Agonist Properties

  title={AMD3100 Is a CXCR7 Ligand with Allosteric Agonist Properties},
  author={Irina Kalatskaya and Yamina A. Berchiche and St{\'e}phanie Gravel and Brian J. Limberg and Jan S. Rosenbaum and Nikolaus Heveker},
  journal={Molecular Pharmacology},
  pages={1240 - 1247}
The bicyclam AMD3100 is known as a small synthetic inhibitor of the CXCL12-binding chemokine receptor CXCR4. Here, we show that AMD3100 also binds to the alternative CXCL12 receptor CXCR7. CXCL12 or AMD3100 alone activate β-arrestin recruitment to CXCR7, which we identify as a previously unreported signaling pathway of CXCR7. In addition, AMD3100 increases CXCL12 binding to CXCR7 and CXCL12-induced conformational rearrangements in the receptor dimer as measured by bioluminescence resonance… 

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