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Updated: Sep 29, 2025
Identification of Transcription Factor Regulators using Medium-Throughput Screening of Arrayed Libraries and a Dual-Luciferase-Based Reporter
Published on: March 27, 2020
Targeting key proteins involved in transcriptional regulation for cancer therapy: Current strategies and future
Haixiang Pei1,2, Weikai Guo2,3, Yangrui Peng2
1Institute for Advanced Study, Shenzhen University and Guangdong Key Laboratory for Biomedical Measurements and Ultrasound Imaging, School of Biomedical Engineering, Shenzhen University Health Science Center, Shenzhen, China.
Abstract:
The key proteins involved in transcriptional regulation play convergent roles in cellular homeostasis, and their dysfunction mediates aberrant gene expressions that underline the hallmarks of tumorigenesis. As tumor progression is dependent on such abnormal regulation of transcription, it is important to discover novel chemical entities as antitumor drugs that target key tumor-associated proteins involved in transcriptional regulation. Despite most key proteins (especially transcription factors) involved in transcriptional regulation are historically recognized as undruggable targets, multiple targeting approaches at diverse levels of transcriptional regulation, such as epigenetic intervention, inhibition of DNA-binding of transcriptional factors, and inhibition of the protein-protein interactions (PPIs), have been established in preclinically or clinically studies. In addition, several new approaches have recently been described, such as targeting proteasomal degradation and eliciting synthetic lethality. This review will emphasize on accentuating these developing therapeutic approaches and provide a thorough conspectus of the drug development to target key proteins involved in transcriptional regulation and their impact on future oncotherapy.
Insights
Targeting proteins in transcriptional regulation is crucial for cancer therapy. This review explores novel drug development strategies for these historically undruggable targets, offering new hope for cancer treatment.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Dysfunctional transcriptional regulation drives cancer development by altering gene expression.
- Key proteins in transcriptional regulation are historically considered challenging, or 'undruggable', cancer targets.
- Targeting these proteins is essential for developing novel antitumor drugs.
Purpose of the Study:
- To review emerging therapeutic strategies for targeting key proteins in transcriptional regulation for cancer treatment.
- To provide a comprehensive overview of drug development targeting transcriptional regulation in oncology.
- To highlight the impact of these approaches on future cancer therapy.
Main Methods:
- Review of preclinical and clinical studies on targeting transcriptional regulation.
- Exploration of diverse targeting strategies including epigenetic intervention, DNA-binding inhibition, and protein-protein interaction (PPI) inhibition.
- Discussion of novel approaches like proteasomal degradation and synthetic lethality.
Main Results:
- Multiple therapeutic strategies are being developed to target key proteins in transcriptional regulation.
- Established and novel approaches show promise in preclinical and clinical settings.
- These strategies offer new avenues for drug development against cancer.
Conclusions:
- Targeting transcriptional regulation represents a promising frontier in cancer therapy.
- Despite challenges, significant progress is being made in developing drugs for these targets.
- These advancements hold potential for transforming future oncotherapy.
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