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Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers
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Drugging the undruggable: transcription therapy for cancer

Chunhong Yan1, Paul J Higgins

  • 1Center for Cell Biology and Cancer Research, Albany Medical College, MC-165, 47 New Scotland Avenue, Albany, NY 12208, USA. yanc@mail.amc.edu

Biochimica Et Biophysica Acta
|November 14, 2012
PubMed

Insights

Cancer cells rely on altered gene expression, making transcriptional regulation a key therapeutic target. New agents targeting transcription factors and epigenetic changes offer promising cancer treatment strategies.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Aberrant gene expression is a hallmark of cancer, driven by oncogenic signaling pathways.
  • Cancer cells often become dependent on this altered transcriptional landscape for survival and proliferation.
  • Transcription, traditionally viewed as 'undruggable,' is increasingly recognized as a viable therapeutic target.

Purpose of the Study:

  • To provide a comprehensive overview of targeting transcriptional regulation for cancer therapy.
  • To discuss strategies for developing transcription-targeted therapeutic agents.
  • To highlight the potential of rectifying cancer-associated transcriptional abnormalities.

Main Methods:

  • Review of existing literature on transcriptional regulation in cancer.
  • Analysis of therapeutic agents targeting DNA binding, protein-protein interactions, and epigenetic modifications.
  • Discussion of artificial transcription factors and reporter assays for drug discovery.

Main Results:

  • Development of agents targeting various levels of transcriptional regulation.
  • Clinical approval or trial entry for several transcription-targeted agents.
  • Advancements in reporter assays facilitating the discovery of new therapeutic agents.

Conclusions:

  • Targeting transcriptional regulation represents a promising therapeutic avenue for cancer treatment.
  • A range of strategies and agents are emerging to address 'undruggable' targets.
  • Further development of transcription-targeted therapies holds significant potential for clinical application.

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