Chemical modulation of transcription factors.
Bianca WiedemannJörn WeisnerDaniel RauhPublished in: MedChemComm (2018)
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.
Keyphrases
- transcription factor
- gene expression
- endothelial cells
- induced apoptosis
- oxidative stress
- signaling pathway
- papillary thyroid
- small molecule
- dna methylation
- dna binding
- lps induced
- cell cycle arrest
- cognitive decline
- cell proliferation
- cell free
- squamous cell
- circulating tumor
- estrogen receptor
- squamous cell carcinoma
- immune response
- genome wide identification
- endoplasmic reticulum stress
- cell death
- childhood cancer
- lymph node metastasis
- drug discovery