Advances in targeting 'undruggable'transcription factors with small molecules

MJ Henley, AN Koehler - Nature Reviews Drug Discovery, 2021 - nature.com
Transcription factors (TFs) represent key biological players in diseases including cancer,
autoimmunity, diabetes and cardiovascular disease. However, outside nuclear receptors …

Targeting transcription factors in cancer

AS Bhagwat, CR Vakoc - Trends in cancer, 2015 - cell.com
Transcription factors (TFs) are commonly deregulated in the pathogenesis of human cancer
and are a major class of cancer cell dependencies. Consequently, targeting of TFs can be …

Targeting post-translational modification of transcription factors as cancer therapy

M Qian, F Yan, T Yuan, B Yang, Q He, H Zhu - Drug Discovery Today, 2020 - Elsevier
Highlights•Transcription factors are generally dysregulated in tumors.•Most oncogenic
transcription factors are considered as “undruggable” targets.•Post-translational …

[HTML][HTML] Drugging the 'undruggable'. Therapeutic targeting of protein–DNA interactions with the use of computer-aided drug discovery methods

M Radaeva, AT Ton, M Hsing, F Ban, A Cherkasov - Drug Discovery Today, 2021 - Elsevier
Transcription factors (TFs) act as major oncodrivers in many cancers and are frequently
regarded as high-value therapeutic targets. The functionality of TFs relies on direct protein …

Transcription factor drug targets

KA Papavassiliou… - Journal of cellular …, 2016 - Wiley Online Library
Transcription factors represent the point of convergence of multiple signaling pathways
within eukaryotic cells. Deregulated transcription factors contribute to the pathogenesis of a …

A complex task? Direct modulation of transcription factors with small molecules

AN Koehler - Current opinion in chemical biology, 2010 - Elsevier
Transcription factors with aberrant activity in disease are promising yet untested targets for
therapeutic development, particularly in oncology. Directly inhibiting or activating the …

Regulation of transcription factor activity by interconnected post-translational modifications

TM Filtz, WK Vogel, M Leid - Trends in pharmacological sciences, 2014 - cell.com
Transcription factors comprise just over 7% of the human proteome and serve as
gatekeepers of cellular function, integrating external signal information into gene expression …

Transcription factors: Bridge between cell signaling and gene regulation

P Weidemüller, M Kholmatov, E Petsalaki… - …, 2021 - Wiley Online Library
Transcription factors (TFs) are key regulators of intrinsic cellular processes, such as
differentiation and development, and of the cellular response to external perturbation …

[HTML][HTML] Pharmacological manipulation of transcription factor protein-protein interactions: opportunities and obstacles

F Fontaine, J Overman… - Cell …, 2015 - cellregeneration.springeropen.com
Much research on transcription factor biology and their genetic pathways has been
undertaken over the last 30 years, especially in the field of developmental biology and …

Proteome-wide profiling of activated transcription factors with a concatenated tandem array of transcription factor response elements

C Ding, DW Chan, W Liu, M Liu, D Li… - Proceedings of the …, 2013 - National Acad Sciences
Transcription factors (TFs) are families of proteins that bind to specific DNA sequences, or TF
response elements (TFREs), and function as regulators of many cellular processes …