Current strategies and progress for targeting the “undruggable” transcription factors
J Zhuang, Q Liu, D Wu, L Tie - Acta Pharmacologica Sinica, 2022 - nature.com
Transcription factors (TFs) specifically bind to DNA, recruit cofactor proteins and modulate
target gene expression, rendering them essential roles in the regulation of numerous …
target gene expression, rendering them essential roles in the regulation of numerous …
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 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 …
Post-translational modification of transcription factors: mechanisms and potential therapeutic interventions
Transcription factors (TFs) orchestrate multiple cellular processes through tight regulation
via post-translational modifications (PTMs). Thus, decoding the combinations of PTMs …
via post-translational modifications (PTMs). Thus, decoding the combinations of PTMs …
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 DNA binding proteins for cancer therapy
Y Shiroma, R Takahashi, Y Yamamoto… - Cancer …, 2020 - Wiley Online Library
Dysregulation or mutation of DNA binding proteins such as transcription factors (TFs) is
associated with the onset and progression of various types of disease, including cancer …
associated with the onset and progression of various types of disease, including cancer …
Transcription factor therapeutics: long-shot or lodestone
D Ghosh, AG Papavassiliou - Current medicinal chemistry, 2005 - ingentaconnect.com
Many drugs, both approved and in development, exert their effects through transcription
factors. The complexity of the biology of transcriptional regulation, however, presents …
factors. The complexity of the biology of transcriptional regulation, however, presents …
Transcription factors in the development and treatment of immune disorders
SD Patalano, P Fuxman Bass, JI Fuxman Bass - Transcription, 2023 - Taylor & Francis
Immune function is highly controlled at the transcriptional level by the binding of transcription
factors (TFs) to promoter and enhancer elements. Several TF families play major roles in …
factors (TFs) to promoter and enhancer elements. Several TF families play major roles in …
Systematic target function annotation of human transcription factors
Abstract Background Transcription factors (TFs), the key players in transcriptional regulation,
have attracted great experimental attention, yet the functions of most human TFs remain …
have attracted great experimental attention, yet the functions of most human TFs remain …
Transcription-factor-modulating agents: precision and selectivity in drug design
AG Papavassiliou - Molecular medicine today, 1998 - cell.com
Transcription factors play an important role in the long-term regulation of cell growth,
differentiation and responses to environmental cues. There is growing evidence that these …
differentiation and responses to environmental cues. There is growing evidence that these …