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Updated: Aug 30, 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 transcription factors in cancer drug discovery
1Institute of Health and Biomedical Innovation, the Queensland University of Technology, Brisbane 4059, Australia.
Abstract:
Cancer drug discovery is currently dominated by clinical trials or clinical research. Several potential drug candidates have been brought into the pipeline of drug discovery after showing very promising results at the pre-clinical level and are waiting to be tested in human clinical trials. Interestingly, among the potential drug candidates, a few of them have targeted transcription factors highlighting the fundamental undruggable nature of these molecules. However, using advanced technologies, researchers were recently successful in partly unlocking this undruggable nature, which was considered as a 'grey area' in the early days of drug discovery, and as a result, several potential candidates have emerged recently. The purpose of the review is to highlight some of the recently reported studies of targeting transcription factors in cancer and their promising outcomes.
Insights
Researchers are developing new cancer drugs targeting transcription factors, previously considered undruggable. Recent advancements show promising pre-clinical results, advancing these novel cancer therapeutics toward clinical trials.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Cancer drug discovery relies heavily on clinical trials and research.
- Transcription factors are historically challenging targets in drug development due to their 'undruggable' nature.
- Recent technological advancements are beginning to overcome these challenges.
Purpose of the Study:
- To review recent studies focused on targeting transcription factors in cancer.
- To highlight the promising outcomes of these novel therapeutic strategies.
Main Methods:
- Literature review of recently reported studies.
- Analysis of pre-clinical data for drug candidates targeting transcription factors.
Main Results:
- Several potential drug candidates targeting transcription factors have emerged.
- These candidates show promising pre-clinical results.
Conclusions:
- Targeting transcription factors is a viable and emerging strategy in cancer drug discovery.
- Advanced technologies are key to unlocking the therapeutic potential of these targets.
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