Targeting EphA3 inhibits cancer growth by disrupting the tumor stromal microenvironment

Cancer Res. 2014 Aug 15;74(16):4470-81. doi: 10.1158/0008-5472.CAN-14-0218.

Abstract

Eph receptor tyrosine kinases are critical for cell-cell communication during normal and oncogenic tissue patterning and tumor growth. Somatic mutation profiles of several cancer genomes suggest EphA3 as a tumor suppressor, but its oncogenic expression pattern and role in tumorigenesis remain largely undefined. Here, we report unexpected EphA3 overexpression within the microenvironment of a range of human cancers and mouse tumor xenografts where its activation inhibits tumor growth. EphA3 is found on mouse bone marrow-derived cells with mesenchymal and myeloid phenotypes, and activation of EphA3(+)/CD90(+)/Sca1(+) mesenchymal/stromal cells with an EphA3 agonist leads to cell contraction, cell-cell segregation, and apoptosis. Treatment of mice with an agonistic α-EphA3 antibody inhibits tumor growth by severely disrupting the integrity and function of newly formed tumor stroma and microvasculature. Our data define EphA3 as a novel target for selective ablation of the tumor microenvironment and demonstrate the potential of EphA3 agonists for anticancer therapy.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antibodies, Monoclonal / pharmacology*
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Cell Transformation, Neoplastic
  • Disease Models, Animal
  • Gene Expression Regulation, Neoplastic
  • HEK293 Cells
  • Humans
  • Mice
  • Mice, Nude
  • Molecular Targeted Therapy
  • Receptor Protein-Tyrosine Kinases / agonists*
  • Receptor Protein-Tyrosine Kinases / biosynthesis*
  • Receptor Protein-Tyrosine Kinases / immunology
  • Receptor Protein-Tyrosine Kinases / metabolism
  • Receptor, EphA3 / agonists*
  • Receptor, EphA3 / biosynthesis*
  • Receptor, EphA3 / immunology
  • Receptor, EphA3 / metabolism
  • Signal Transduction
  • Stromal Cells / drug effects
  • Stromal Cells / pathology
  • Tumor Microenvironment / drug effects

Substances

  • Antibodies, Monoclonal
  • EPHA3 protein, human
  • Epha3 protein, mouse
  • Receptor Protein-Tyrosine Kinases
  • Receptor, EphA3