A Novel Approach to the Development of Highly Specific Inhibitors of EFG, a Critical Transcription Factor in Prostate Cancer

Abstract

We have created a series of six constructs to express varying length fragments of ERG. Expression and purification protocols have been established for all six fragments. Using fluorescein-labeled oligonucleotides, we have developed a fluorescence polarization based assay for measuring the DNA binding of the ERG fragments to a functional DNA element. Using this assay, we have shown that longer fragments of ERG show decreased DNA binding, i.e. are auto-inhibited. Based on this data, we have focused efforts on producing one fragment in the labeled form necessary for NMR structural studies.

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Document Details

Document Type
Technical Report
Publication Date
Mar 01, 2008
Accession Number
ADA482921

Entities

People

  • John H. Bushweller
  • Tomasz K. Kabzinski

Organizations

  • University of Virginia

Tags

DTIC Thesaurus Topics

  • Amino Acids
  • Biomedical Research
  • Department Of Defense
  • Fluorescence
  • Inhibition
  • Inhibitors
  • Laser Dyes
  • Lead Compounds
  • Low Temperature
  • Magnetic Resonance
  • Measurement
  • Nuclear Magnetic Resonance
  • Polarization
  • Prostate
  • Prostate Cancer
  • Transcription Factors
  • United States

Fields of Study

  • Biology
  • Chemistry

Readers

  • Molecular Genetics
  • Molecular and Cellular Biochemistry
  • Molecular and genetic basis of cancer.