Related Experiment Video

Updated: Apr 24, 2026

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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Identification of small molecule modulators of gene transcription with anticancer activity

Tram Anh Tran1, Jennifer Wichterman-Kouznetsova, Diana Varghese

  • 1Hamon Center for Therapeutic Oncology Research and ∥Department of Pharmacology, University of Texas Southwestern Medical Center , Dallas, Texas 75390, United States.

ACS Chemical Biology
|September 5, 2014
PubMed

Insights

Researchers identified 19 novel small molecules that regulate gene expression and impact cell growth. Two compounds selectively target cancer cells, offering potential for new epigenetic therapies.

Area of Science:

  • Molecular Biology
  • Epigenetics
  • Chemical Biology

Background:

  • Epigenetic gene regulation is crucial for biological processes.
  • Dysregulation of epigenetics contributes to diseases like cancer.

Purpose of the Study:

  • To identify novel small molecules regulating gene expression using a high-throughput screening assay.
  • To find compounds that can modulate epigenetic mechanisms for therapeutic potential.

Main Methods:

  • Utilized an image-based Locus Derepression assay for quantitative high-throughput screening of 283,122 compounds.
  • Validated identified compounds through confirmation and independent testing.
  • Assessed anti-proliferative activity and cancer cell selectivity.

Main Results:

  • Identified 19 small molecules that induce reporter gene expression over 2-fold.
  • 17 compounds exhibited anti-proliferative effects.
  • Two compounds demonstrated cancer cell selectivity and altered histone marks.

Conclusions:

  • The identified compounds are valuable chemical tools for studying epigenetic regulation of transcription.
  • These molecules offer potential for developing new strategies to modulate cell growth pathways in cancer.

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