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Updated: Mar 29, 2026

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
Anand S Bhagwat1, Christopher R Vakoc1
1Cold Spring Harbor Laboratory, 1 Bungtown Road, Cold Spring Harbor, NY 11724, USA.
Abstract:
Transcription factors (TFs) are commonly deregulated in the pathogenesis of human cancer and are a major class of cancer cell dependencies. Consequently, targeting of TFs can be highly effective in treating particular malignancies, as highlighted by the clinical efficacy of agents that target nuclear hormone receptors. In this review we discuss recent advances in our understanding of TFs as drug targets in oncology, with an emphasis on the emerging chemical approaches to modulate TF function. The remarkable diversity and potency of TFs as drivers of cell transformation justifies a continued pursuit of TFs as therapeutic targets for drug discovery.
Insights
Transcription factors (TFs) are key drivers of cancer. Targeting these crucial proteins offers a promising therapeutic strategy for various malignancies, with ongoing research into novel chemical approaches for drug discovery.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Transcription factors (TFs) are frequently dysregulated in human cancer.
- Cancer cells often depend on these deregulated TFs for survival and proliferation.
- Targeting TFs has shown clinical success, exemplified by therapies against nuclear hormone receptors.
Purpose of the Study:
- To review recent advancements in understanding TFs as drug targets in oncology.
- To highlight emerging chemical strategies for modulating TF activity.
- To emphasize the therapeutic potential of TFs in cancer drug discovery.
Main Methods:
- Literature review of recent scientific publications.
- Analysis of emerging chemical approaches for TF modulation.
- Discussion of TF roles in cancer pathogenesis and therapeutic targeting.
Main Results:
- TFs are critical regulators of gene expression in cancer.
- Targeting TFs can lead to effective cancer treatments.
- Novel chemical strategies are being developed to modulate TF function.
Conclusions:
- Transcription factors represent a significant class of therapeutic targets in oncology.
- The development of chemical agents to modulate TF function is a rapidly advancing field.
- Continued research into TFs is essential for discovering new cancer drugs.
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