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 …

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 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 …

Post-translational modification of transcription factors: mechanisms and potential therapeutic interventions

SL Planey, R Kumar, JA Arnott - Current Molecular …, 2013 - ingentaconnect.com
Transcription factors (TFs) orchestrate multiple cellular processes through tight regulation
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 …

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 …

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 …

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 …

Systematic target function annotation of human transcription factors

YF Li, RB Altman - BMC biology, 2018 - Springer
Abstract Background Transcription factors (TFs), the key players in transcriptional regulation,
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 …