Chemical modulation of transcription factors

MedChemComm
Bianca WiedemannDaniel Rauh

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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Feb 12, 2020·Seminars in Cancer Biology·Dominique R PerezKsenia Matlawska-Wasowska
Oct 29, 2020·Nature Communications·Hélène AdihouHerbert Waldmann
Jan 14, 2021·International Journal of Biological Macromolecules·Marjan TalebiSaeed Samarghandian

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Methods Mentioned

BETA
X-ray
acetylation
co-immunoprecipitation
ELISA
two-hybrid
xenografts
ubiquitination
nuclear translocation
AlphaScreen
FRET

Clinical Trials Mentioned

NCT02909972
NCT02264613

Software Mentioned

stattic
AlphaScreen
iOS

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