Enhanced sensitivity to IGF-II signaling links loss of imprinting of IGF2 to increased cell proliferation and tumor risk

Proc Natl Acad Sci U S A. 2007 Dec 26;104(52):20926-31. doi: 10.1073/pnas.0710359105. Epub 2007 Dec 17.

Abstract

Loss of imprinting (LOI) of the insulin-like growth factor-II gene (IGF2), leading to abnormal activation of the normally silent maternal allele, is a common human epigenetic population variant associated with a 5-fold increased frequency of colorectal neoplasia. Here, we show first that LOI leads specifically to increased expression of proliferation-related genes in mouse intestinal crypts. Surprisingly, LOI(+) mice also have enhanced sensitivity to IGF-II signaling, not simply increased IGF-II levels, because in vivo blockade with NVP-AEW541, a specific inhibitor of the IGF-II signaling receptor, showed reduction of proliferation-related gene expression to levels half that seen in LOI(-) mice. Signal transduction assays in microfluidic chips confirmed this enhanced sensitivity with marked augmentation of Akt/PKB signaling in LOI(+) cells at low doses of IGF-II, which was reduced in the presence of the inhibitor to levels below those found in LOI(-) cells, and was associated with increased expression of the IGF1 and insulin receptor genes. We exploited this increased IGF-II sensitivity to develop an in vivo chemopreventive strategy using the azoxymethane (AOM) mutagenesis model. LOI(+) mice treated with AOM showed a 60% increase in premalignant aberrant crypt foci (ACF) formation over LOI(-) mice. In vivo IGF-II blockade with NVP-AEW541 abrogated this effect, reducing ACF to a level 30% lower even than found in exposed LOI(-) mice. Thus, LOI increases cancer risk in a counterintuitive way, by increasing the sensitivity of the IGF-II signaling pathway itself, providing a previously undescribed epigenetic chemoprevention strategy in which cells with LOI are "IGF-II addicted" and undergo reduced tumorigenesis in the colon upon IGF-II pathway blockade.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, N.I.H., Intramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anticarcinogenic Agents / pharmacology
  • Azoxymethane / pharmacology
  • Cell Proliferation
  • DNA Methylation
  • Epigenesis, Genetic
  • Gene Expression Regulation, Neoplastic
  • Genomic Imprinting*
  • Insulin-Like Growth Factor II / genetics*
  • Insulin-Like Growth Factor II / metabolism*
  • Mice
  • Mice, Inbred C57BL
  • Neoplasms / genetics*
  • Neoplasms / metabolism*
  • Oligonucleotide Array Sequence Analysis
  • Pyrimidines / pharmacology
  • Pyrroles / pharmacology
  • Signal Transduction

Substances

  • Anticarcinogenic Agents
  • NVP-AEW541
  • Pyrimidines
  • Pyrroles
  • Insulin-Like Growth Factor II
  • Azoxymethane

Associated data

  • GEO/GSE8583