Related Experiment Video

Updated: Dec 18, 2025

Identification of Transcription Factor Regulators using Medium-Throughput Screening of Arrayed Libraries and a Dual-Luciferase-Based Reporter
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Identification of Transcription Factor Regulators using Medium-Throughput Screening of Arrayed Libraries and a Dual-Luciferase-Based Reporter

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Targeting post-translational modification of transcription factors as cancer therapy

Meijia Qian1, Fangjie Yan1, Tao Yuan1

  • 1Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.

Drug Discovery Today
|June 17, 2020
PubMed

Insights

Transcription factors (TFs) drive cancer by altering gene expression. Targeting their post-translational modifications (PTMs) offers new therapeutic strategies for

Area of Science:

  • Oncology and Molecular Biology: Focuses on the role of transcription factors and their modifications in cancer development and treatment.

Background:

  • Dysregulated transcription factors (TFs) are key drivers of cancer, promoting uncontrolled cell growth, migration, and immune evasion.
  • Most TFs are considered 'undruggable' due to challenges in directly modulating their activity.
  • Post-translational modifications (PTMs) critically regulate TF functions, presenting alternative therapeutic targets.

Purpose of the Study:

  • To systematically review emerging concepts and agents targeting PTMs of TFs in cancer.
  • To explore the potential of PTM-associated TF targeting as a novel paradigm for cancer therapy.

Main Methods:

  • Comprehensive literature review of PTMs affecting TF activity and their role in cancer.
  • Analysis of current and emerging therapeutic strategies targeting TF PTMs.
  • Synthesis of findings to highlight potential treatment paradigms.

Main Results:

  • PTMs significantly influence TF localization, interactions, and stability, thereby controlling gene expression networks in cancer.
  • Targeting specific TF PTMs offers a promising strategy to overcome the 'undruggable' nature of many TFs.
  • Emerging agents demonstrate potential in modulating PTMs for therapeutic benefit.

Conclusions:

  • PTM-associated TF targeting represents a promising frontier in cancer therapy.
  • Further research into PTMs could unlock new treatments for various cancers.
  • This review provides a framework for developing novel TF-targeted cancer therapies.

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