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 …
The roles of histone deacetylases and their inhibitors in cancer therapy
G Li, Y Tian, WG Zhu - Frontiers in cell and developmental biology, 2020 - frontiersin.org
Genetic mutations and abnormal gene regulation are key mechanisms underlying
tumorigenesis. Nucleosomes, which consist of DNA wrapped around histone cores …
tumorigenesis. Nucleosomes, which consist of DNA wrapped around histone cores …
Current and future treatment strategies for rhabdomyosarcoma
Rhabdomyosarcoma (RMS) is the most common soft tissue sarcoma in children, and can be
subcategorized histologically and/or based on PAX-FOXO1 fusion gene status. Over the last …
subcategorized histologically and/or based on PAX-FOXO1 fusion gene status. Over the last …
Targeting histone acetylation dynamics and oncogenic transcription by catalytic P300/CBP inhibition
To separate causal effects of histone acetylation on chromatin accessibility and
transcriptional output, we used integrated epigenomic and transcriptomic analyses following …
transcriptional output, we used integrated epigenomic and transcriptomic analyses following …
HDAC inhibitors elicit metabolic reprogramming by targeting super-enhancers in glioblastoma models
TTT Nguyen, Y Zhang, E Shang, C Shu… - The Journal of …, 2020 - Am Soc Clin Investig
The Warburg effect is a tumor-related phenomenon that could potentially be targeted
therapeutically. Here, we showed that glioblastoma (GBM) cultures and patients' tumors …
therapeutically. Here, we showed that glioblastoma (GBM) cultures and patients' tumors …
Histone hyperacetylation disrupts core gene regulatory architecture in rhabdomyosarcoma
Core regulatory transcription factors (CR TFs) orchestrate the placement of super-enhancers
(SEs) to activate transcription of cell-identity specifying gene networks, and are critical in …
(SEs) to activate transcription of cell-identity specifying gene networks, and are critical in …
Transcriptional regulation by (super) enhancers: from discovery to mechanisms
F Grosveld, J van Staalduinen… - Annual review of …, 2021 - annualreviews.org
Accurate control of gene expression in the right cell at the right moment is of fundamental
importance to animal development and homeostasis. At the heart of gene regulation lie the …
importance to animal development and homeostasis. At the heart of gene regulation lie the …
Discovery of histone deacetylase 3 (HDAC3)-specific PROTACs
Histone deacetylases (HDACs) are validated drug targets for cancer treatment. Increased
HDAC isozyme selectivity and novel strategies to inhibit HDAC activity could lead to safer …
HDAC isozyme selectivity and novel strategies to inhibit HDAC activity could lead to safer …
Now open: evolving insights to the roles of lysine acetylation in chromatin organization and function
Protein acetylation is conserved across phylogeny and has been recognized as one of the
most prominent post-translational modifications since its discovery nearly 60 years ago …
most prominent post-translational modifications since its discovery nearly 60 years ago …
Trends and potential of machine learning and deep learning in drug study at single-cell level
Cancer treatments always face challenging problems, particularly drug resistance due to
tumor cell heterogeneity. The existing datasets include the relationship between gene …
tumor cell heterogeneity. The existing datasets include the relationship between gene …