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Updated: Feb 6, 2026
High-throughput Screening for Chemical Modulators of Post-transcriptionally Regulated Genes
Published on: March 3, 2015
Chemical modulation of transcription factors
Bianca Wiedemann1, Jörn Weisner1, Daniel Rauh1
1Technische Universität Dortmund , Fakultät für Chemie und Chemische Biologie , Otto-Hahn-Strasse 4a , D-44227 Dortmund , Germany . Email: daniel.rauh@tu-dortmund.de ; ; Tel: +49 (0)231 755 7080.
Abstract:
Transcription factors (TFs) constitute a diverse class of sequence-specific DNA-binding proteins, which are key to the modulation of gene expression. TFs have been associated with human diseases, including cancer, Alzheimer's and other neurodegenerative diseases, which makes this class of proteins attractive targets for chemical biology and medicinal chemistry research. Since TFs lack a common binding site or structural similarity, the development of small molecules to efficiently modulate TF biology in cells and in vivo is a challenging task. This review highlights various strategies that are currently being explored for the identification and development of modulators of Myc, p53, Stat, Nrf2, CREB, ER, AR, HIF, NF-κB, and BET proteins.
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