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Issue 8, 2018
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Chemical modulation of transcription factors

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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.

Graphical abstract: Chemical modulation of transcription factors

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Article information

30 May 2018
10 Jul 2018
First published
11 Jul 2018

Med. Chem. Commun., 2018,9, 1249-1272
Article type
Review Article

Chemical modulation of transcription factors

B. Wiedemann, J. Weisner and D. Rauh, Med. Chem. Commun., 2018, 9, 1249
DOI: 10.1039/C8MD00273H

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