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 …
[HTML][HTML] Reading the chromatinized genome
AK Michael, NH Thomä - Cell, 2021 - cell.com
Eukaryotic DNA-binding proteins operate in the context of chromatin, where nucleosomes
are the elementary building blocks. Nucleosomal DNA is wrapped around a histone core …
are the elementary building blocks. Nucleosomal DNA is wrapped around a histone core …
Mammalian SWI/SNF continuously restores local accessibility to chromatin
M Iurlaro, MB Stadler, F Masoni, Z Jagani, GG Galli… - Nature …, 2021 - nature.com
Chromatin accessibility is a hallmark of regulatory regions, entails transcription factor (TF)
binding and requires nucleosomal reorganization. However, it remains unclear how …
binding and requires nucleosomal reorganization. However, it remains unclear how …
BANP opens chromatin and activates CpG-island-regulated genes
The majority of gene transcripts generated by RNA polymerase II in mammalian genomes
initiate at CpG island (CGI) promoters,, yet our understanding of their regulation remains …
initiate at CpG island (CGI) promoters,, yet our understanding of their regulation remains …
[HTML][HTML] SPT5 stabilizes RNA polymerase II, orchestrates transcription cycles, and maintains the enhancer landscape
Transcription progression is governed by multitasking regulators including SPT5, an
evolutionarily conserved factor implicated in virtually all transcriptional steps from enhancer …
evolutionarily conserved factor implicated in virtually all transcriptional steps from enhancer …
Dissecting OCT4 defines the role of nucleosome binding in pluripotency
GA Roberts, B Ozkan, I Gachulincová, MR O'Dwyer… - Nature cell …, 2021 - nature.com
Pioneer transcription factors such as OCT4 can target silent genes embedded in
nucleosome-dense regions. How nucleosome interaction enables transcription factors to …
nucleosome-dense regions. How nucleosome interaction enables transcription factors to …
Chemical inhibition of ENL/AF9 YEATS domains in acute leukemia
L Garnar-Wortzel, TR Bishop, S Kitamura… - ACS central …, 2021 - ACS Publications
Transcriptional coregulators, which mediate chromatin-dependent transcriptional signaling,
represent tractable targets to modulate tumorigenic gene expression programs with small …
represent tractable targets to modulate tumorigenic gene expression programs with small …
[HTML][HTML] A BRD4-mediated elongation control point primes transcribing RNA polymerase II for 3′-processing and termination
M Arnold, A Bressin, O Jasnovidova, D Meierhofer… - Molecular Cell, 2021 - cell.com
Transcription elongation has emerged as a regulatory hub in gene expression of
metazoans. A major control point occurs during early elongation before RNA polymerase II …
metazoans. A major control point occurs during early elongation before RNA polymerase II …
[HTML][HTML] Acute depletion of the ARID1A subunit of SWI/SNF complexes reveals distinct pathways for activation and repression of transcription
S Blümli, N Wiechens, MY Wu, V Singh, M Gierlinski… - Cell reports, 2021 - cell.com
The ARID1A subunit of SWI/SNF chromatin remodeling complexes is a potent tumor
suppressor. Here, a degron is applied to detect rapid loss of chromatin accessibility at …
suppressor. Here, a degron is applied to detect rapid loss of chromatin accessibility at …
FUS oncofusion protein condensates recruit mSWI/SNF chromatin remodeler via heterotypic interactions between prion‐like domains
Fusion transcription factors generated by genomic translocations are common drivers of
several types of cancers including sarcomas and leukemias. Oncofusions of the FET (FUS …
several types of cancers including sarcomas and leukemias. Oncofusions of the FET (FUS …