Evaluation of Molecular Inhibitors of the c-Myc Oncoprotein

Abstract

c-Myc is a bHLH-ZIP transcription factor that regulates the expression of a large number of target genes, which collectively promote transformation. The active form of c-Myc exists as a heterodimer with another bHLH-ZIP protein, Max. This interaction, along with c-Myc-Max sequence-specific DNA binding ability is necessary for all of c-Myc's biological properties, including transformation. The factors which make c-Myc a compelling therapeutic target have recently been reviewed. Also addressed were the various levels at which pharmacologic attacks upon c-Myc, other members of the c-Myc network, or c-Myc target genes might be aimed. Among the strategies thus far employed (with limited success) are the targeting of the CMYC gene with triplex-forming oligonucleotides, the use of anti-sense oligonucleotides to target c-Myc mRNA, the use of short, double-stranded E-box containing oligonucleotides that serve as decoy binding sites, and the use of dominant-negative forms of c-Myc. The strengths and limitations of these approaches were discussed at length in this review.

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Document Details

Document Type
Technical Report
Publication Date
Feb 01, 2007
Accession Number
ADA475799

Entities

People

  • Edward Prochownik

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DTIC Thesaurus Topics

  • Albumins
  • Amino Acids
  • Cell Line
  • Chemical Synthesis
  • Chemistry
  • Free Energy
  • Genetics
  • Health Services
  • Liquid Chromatography
  • Magnetic Resonance
  • Molecular Weight
  • Neoplasms
  • Nuclear Magnetic Resonance
  • Proteins
  • Therapy
  • Three Dimensional
  • Transcription Factors

Fields of Study

  • Chemistry

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  • Molecular Genetics
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