Indole-3-carbinol disrupts estrogen receptor-alpha dependent expression of insulin-like growth factor-1 receptor and insulin receptor substrate-1 and proliferation of human breast cancer cells

Mol Cell Endocrinol. 2012 Nov 5;363(1-2):74-84. doi: 10.1016/j.mce.2012.07.008. Epub 2012 Jul 24.

Abstract

We previously established that Indole-3-Carbinol (I3C), a natural hydrolysis product of glucobrassicin in cruciferous vegetables, arrests the proliferation of estrogen-dependent human breast cancer cells and induces protein degradation of Estrogen Receptor-alpha (ERα). We demonstrate in human MCF-7 breast cancer cells that I3C ablates expression of Insulin-like Growth Factor Receptor-1 (IGF1R) and Insulin Receptor Substrate-1 (IRS1), downstream effectors of the IGF1 signaling pathway. Exogenous ERα reversed the I3C mediated loss of IGF1R and IRS1 gene expression demonstrating that down-regulation of ERα is functionally linked to I3C control of IGF1R and IRS1 expression. I3C disrupted binding of endogenous ERα, but not Sp1, to ERE-Sp1 composite elements within the IGF1R/IRS1 promoters. Exogenous ERα abrogated, and combined expression of IGF1R and IRS1 attenuated, the I3C mediated cell cycle arrest. Therefore, I3C inhibits proliferation of estrogen-sensitive breast cancer cells through disruption of ERα-mediated transcription of cell signaling components within the IGF1 cascade.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents, Phytogenic / pharmacology*
  • Base Sequence
  • Breast Neoplasms
  • Cell Proliferation / drug effects*
  • Conserved Sequence
  • Dose-Response Relationship, Drug
  • Estradiol / pharmacology
  • Estradiol / physiology
  • Estrogen Receptor alpha / antagonists & inhibitors
  • Estrogen Receptor alpha / physiology*
  • Estrogens / pharmacology
  • Estrogens / physiology
  • Female
  • G1 Phase Cell Cycle Checkpoints / drug effects
  • Gene Expression / drug effects
  • Gene Expression Regulation, Neoplastic
  • Humans
  • Indoles / pharmacology*
  • Insulin Receptor Substrate Proteins / genetics
  • Insulin Receptor Substrate Proteins / metabolism*
  • MCF-7 Cells
  • Molecular Sequence Data
  • Promoter Regions, Genetic
  • Protein Binding
  • Receptor, IGF Type 1 / genetics
  • Receptor, IGF Type 1 / metabolism*
  • Signal Transduction

Substances

  • Antineoplastic Agents, Phytogenic
  • ESR1 protein, human
  • Estrogen Receptor alpha
  • Estrogens
  • IRS1 protein, human
  • Indoles
  • Insulin Receptor Substrate Proteins
  • Estradiol
  • indole-3-carbinol
  • Receptor, IGF Type 1