R1507, an anti-insulin-like growth factor-1 receptor (IGF-1R) antibody, and EWS/FLI-1 siRNA in Ewing's sarcoma: convergence at the IGF/IGFR/Akt axis

PLoS One. 2011;6(10):e26060. doi: 10.1371/journal.pone.0026060. Epub 2011 Oct 11.

Abstract

A subset of patients with Ewing's sarcoma responds to anti-insulin-like growth factor-1 receptor (IGF-1R) antibodies. Mechanisms of sensitivity and resistance are unknown. We investigated whether an anti-IGF-1R antibody acts via a pathway that could also be suppressed by small interfering (si) RNA against the EWS/FLI-1 fusion protein, the hallmark of Ewing's sarcoma. The growth of two Ewing's sarcoma cell lines (TC-32 and TC-71) was inhibited by the fully human anti-IGF-1R antibody, R1507 (clonogenic and MTT assays). TC-32 and TC-71 cells express high levels of IGF-2, while RD-ES and A4573 Ewing's cell lines, which were less responsive to R1507 in our assays, express low or undetectable IGF-2, respectively. TC-71 cells also expressed high levels of IGF-1R, and R1507 decreased steady-state levels of this receptor by internalization/degradation, an effect which was associated with a decrease in p-IGF-1R, p-IRS-1, and p-Akt. EWS/FLI-1 siRNA also decreased p-Akt, due to its ability to increase IGF-BP3 levels and subsequently decrease IGF-1 and IGF-2 levels, thus inhibiting signaling through p-IGF-1R. This inhibition correlated with growth suppression and apoptosis. The attenuation of Akt activation was confirmed in TC-71 and HEK-293 (human embryonic kidney) cells by transfecting them with IGF-1R siRNA. We conclude that antibodies and siRNA to IGF-1R, as well as siRNA to EWS/FLI-1, act via intersecting IGF/IGF-1R signals that suppress a common point in this pathway, namely the phosphorylation of Akt.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Antibodies, Monoclonal / pharmacology*
  • Antibodies, Monoclonal, Humanized
  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Colony-Forming Units Assay
  • Down-Regulation / drug effects
  • HEK293 Cells
  • Humans
  • Insulin Receptor Substrate Proteins / metabolism
  • Insulin-Like Growth Factor Binding Protein 3 / metabolism
  • Insulin-Like Growth Factor II / metabolism
  • Oncogene Proteins, Fusion / metabolism*
  • Phosphorylation / drug effects
  • Polymorphism, Genetic
  • Protein Structure, Tertiary
  • Proto-Oncogene Protein c-fli-1 / metabolism*
  • Proto-Oncogene Proteins c-akt / metabolism*
  • RNA, Small Interfering / metabolism*
  • RNA-Binding Protein EWS / metabolism*
  • Receptor, IGF Type 1 / antagonists & inhibitors*
  • Receptor, IGF Type 1 / metabolism
  • Receptor, IGF Type 2 / chemistry
  • Receptor, IGF Type 2 / genetics
  • Reproducibility of Results
  • Sarcoma, Ewing / metabolism*
  • Signal Transduction / drug effects
  • Somatomedins / metabolism*
  • Transfection

Substances

  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • EWS-FLI fusion protein
  • IGFBP3 protein, human
  • IRS1 protein, human
  • Insulin Receptor Substrate Proteins
  • Insulin-Like Growth Factor Binding Protein 3
  • Oncogene Proteins, Fusion
  • Proto-Oncogene Protein c-fli-1
  • RNA, Small Interfering
  • RNA-Binding Protein EWS
  • Receptor, IGF Type 2
  • Somatomedins
  • Insulin-Like Growth Factor II
  • Receptor, IGF Type 1
  • Proto-Oncogene Proteins c-akt
  • teprotumumab