Small Molecule Inhibitors of ERG and ETV1 in Prostate Cancer

Abstract

The research involves laboratory studies utilizing xenograft models to test the hypothesis that targeting a member of the ETS transcription factor family with small molecules such as YK-4-279 may effectively treat prostate cancer. In year three, Dr. Morrissey was to evaluate the anti-tumor effect of the S-enantiomer of YK-4-279 on 4 human prostate xenograft lines subcutaneously and 2 lines intra-tibial. Dr. Uren supplied Dr. Morrissey with the required compound. The S-enantiomer of YK-4-279 had no significant effect on tumor growth on the first and second ERG+ xenograft. It had an effect on the third ERG+ xenograft line, and no effect on the control xenograft line. A gene expression analysis of the first study suggested a change in the expression of epithelial-mesenchymal transition associated genes in ERG treated tumors. However, immunohistochemical analyses of these proteins in the tumors of treated and untreated animals suggested the change in expression only occurred in a subset of cells within the tumors. Dr. Uren has met with and Skyped with Dr. Morrissey to ensure continued collaboration. We are currently completing a study on the effect of the S-enantiomer of YK-4-279 on intra-tibial tumors and have requested a no cost extension to complete the intra-tibial animal studies.

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Document Details

Document Type
Technical Report
Publication Date
Sep 01, 2015
Accession Number
AD1002720

Entities

People

  • Colm Morrissey

Organizations

  • University of Washington

Tags

DTIC Thesaurus Topics

  • Biomedical Research
  • Body Weight
  • Cancer
  • Cell Line
  • Cells
  • Enantiomers
  • Gene Expression
  • Inhibition
  • Inhibitors
  • Molecules
  • Neoplasms
  • Prostate
  • Prostate Cancer
  • Proteins
  • Small Molecules
  • Tissues
  • Transcription Factors

Readers

  • Military Mobilization and Reserve Forces Studies.
  • Molecular and genetic basis of cancer.
  • Oncology (Cancer Research).