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 …
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 …
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 …
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
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 …
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 …
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 …
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 …
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 …
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 …
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 …
response elements (TFREs), and function as regulators of many cellular processes …
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