Inhibition of CXCR4-CXCL12 chemotaxis in melanoma by AMD11070

Br J Cancer. 2013 Apr 30;108(8):1634-40. doi: 10.1038/bjc.2013.124. Epub 2013 Mar 28.

Abstract

Background: Despite intensive research and novel adjuvant therapies, there is currently no cure for metastatic melanoma. The chemokine receptor CXCR4 controls metastasis to sites such as the liver; however, the therapeutic blockade with the existing agents has proven difficult.

Methods: AMD11070, a novel orally bioavailable inhibitor of CXCR4, was tested for its ability to inhibit the migration of melanoma cells compared with the commonly described antagonist AMD3100.

Results: AMD11070 abrogated melanoma cell migration and was significantly more effective than AMD3100. Importantly for the clinical context, the expression of B-RAF-V600E did not the affect the sensitivity of AMD11070.

Conclusion: Liver-resident myofibroblasts excrete CXCL12, which is able to promote the migration of CXCR4-expressing tumour cells from the blood into the liver. Blockade of this axis by AMD11070 thus represents a novel therapeutic strategy for both B-RAF wild-type and mutated melanomas.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminoquinolines / pharmacology*
  • Benzimidazoles / pharmacology*
  • Butylamines
  • Cell Line, Tumor
  • Cell Migration Inhibition / drug effects*
  • Chemokine CXCL12 / antagonists & inhibitors*
  • Flow Cytometry
  • Heterocyclic Compounds, 1-Ring
  • Humans
  • Liver Neoplasms / secondary
  • Melanoma / drug therapy*
  • Melanoma / pathology*
  • Receptors, CXCR4 / antagonists & inhibitors*

Substances

  • Aminoquinolines
  • Benzimidazoles
  • Butylamines
  • CXCL12 protein, human
  • CXCR4 protein, human
  • Chemokine CXCL12
  • Heterocyclic Compounds, 1-Ring
  • Receptors, CXCR4
  • mavorixafor