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 …
Sarcoma treatment in the era of molecular medicine
Sarcomas are heterogeneous and clinically challenging soft tissue and bone cancers.
Although constituting only 1% of all human malignancies, sarcomas represent the second …
Although constituting only 1% of all human malignancies, sarcomas represent the second …
A first-generation pediatric cancer dependency map
Exciting therapeutic targets are emerging from CRISPR-based screens of high mutational-
burden adult cancers. A key question, however, is whether functional genomic approaches …
burden adult cancers. A key question, however, is whether functional genomic approaches …
TP63, SOX2, and KLF5 establish a core regulatory circuitry that controls epigenetic and transcription patterns in esophageal squamous cell carcinoma cell lines
Background & Aims We investigated the transcriptome of esophageal squamous cell
carcinoma (ESCC) cells, activity of gene regulatory (enhancer and promoter regions), and …
carcinoma (ESCC) cells, activity of gene regulatory (enhancer and promoter regions), and …
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 …
RNA polymerase II is required for spatial chromatin reorganization following exit from mitosis
Mammalian chromosomes are three-dimensional entities shaped by converging and
opposing forces. Mitotic cell division induces marked chromosome condensation, but …
opposing forces. Mitotic cell division induces marked chromosome condensation, but …
The ETS transcription factor ETV6 constrains the transcriptional activity of EWS–FLI to promote Ewing sarcoma
Transcription factors (TFs) are frequently mutated in cancer. Paediatric cancers exhibit few
mutations genome-wide but frequently harbour sentinel mutations that affect TFs, which …
mutations genome-wide but frequently harbour sentinel mutations that affect TFs, which …
ETV6 dependency in Ewing sarcoma by antagonism of EWS-FLI1-mediated enhancer activation
The EWS-FLI1 fusion oncoprotein deregulates transcription to initiate the paediatric cancer
Ewing sarcoma. Here we used a domain-focused CRISPR screen to implicate the …
Ewing sarcoma. Here we used a domain-focused CRISPR screen to implicate the …
A phenotypic screening platform for identifying chemical modulators of astrocyte reactivity
BLL Clayton, JD Kristell, KC Allan, EF Cohn… - Nature …, 2024 - nature.com
Disease, injury and aging induce pathological reactive astrocyte states that contribute to
neurodegeneration. Modulating reactive astrocytes therefore represent an attractive …
neurodegeneration. Modulating reactive astrocytes therefore represent an attractive …
CRISPR/Cas-based epigenome editing: advances, applications, and clinical utility
JH Goell, IB Hilton - Trends in Biotechnology, 2021 - cell.com
The epigenome dynamically regulates gene expression and guides cellular differentiation
throughout the lifespan of eukaryotic organisms. Recent advances in clustered regularly …
throughout the lifespan of eukaryotic organisms. Recent advances in clustered regularly …