Drugging the undruggable: Transcription therapy for cancer

Chunhong Yan, Paul J. Higgins

Research output: Contribution to journalReview articlepeer-review

95 Scopus citations


Transcriptional regulation is often the convergence point of oncogenic signaling. It is not surprising, therefore, that aberrant gene expression is a hallmark of cancer. Transformed cells often develop a dependency on such a reprogramming highlighting the therapeutic potential of rectifying cancer-associated transcriptional abnormalities in malignant cells. Although transcription is traditionally considered as undruggable, agents have been developed that target various levels of transcriptional regulation including DNA binding by transcription factors, protein-protein interactions, and epigenetic alterations. Some of these agents have been approved for clinical use or entered clinical trials. While artificial transcription factors have been developed that can theoretically modulate expression of any given gene, the emergence of reliable reporter assays greatly facilitates the search for transcription-targeted agents. This review provides a comprehensive overview of these developments, and discusses various strategies applicable for developing transcription-targeted therapeutic agents.

Original languageEnglish (US)
Pages (from-to)76-85
Number of pages10
JournalBiochimica et Biophysica Acta - Reviews on Cancer
Issue number1
StatePublished - Jan 2013
Externally publishedYes


  • Cancer
  • Drug development
  • Targeted therapy
  • Transcription
  • Transcription therapy
  • Transcriptional regulation

ASJC Scopus subject areas

  • Oncology
  • Genetics
  • Cancer Research


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