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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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The article was received on 30 May 2018, accepted on 10 Jul 2018 and first published on 11 Jul 2018

Article type: Review Article
DOI: 10.1039/C8MD00273H
Med. Chem. Commun., 2018,9, 1249-1272

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    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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