Chemistries of bifunctional PROTAC degraders
C Cao, M He, L Wang, Y He, Y Rao - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …
Context-specific Polycomb mechanisms in development
JJ Kim, RE Kingston - Nature Reviews Genetics, 2022 - nature.com
Polycomb group (PcG) proteins are crucial chromatin regulators that maintain repression of
lineage-inappropriate genes and are therefore required for stable cell fate. Recent advances …
lineage-inappropriate genes and are therefore required for stable cell fate. Recent advances …
Activity-by-contact model of enhancer–promoter regulation from thousands of CRISPR perturbations
Enhancer elements in the human genome control how genes are expressed in specific cell
types and harbor thousands of genetic variants that influence risk for common diseases …
types and harbor thousands of genetic variants that influence risk for common diseases …
An androgen receptor switch underlies lineage infidelity in treatment-resistant prostate cancer
Cancers adapt to increasingly potent targeted therapies by reprogramming their phenotype.
Here we investigated such a phenomenon in prostate cancer, in which tumours can escape …
Here we investigated such a phenomenon in prostate cancer, in which tumours can escape …
Regulation of gene transcription by Polycomb proteins
S Aranda, G Mas, L Di Croce - Science advances, 2015 - science.org
The Polycomb group (PcG) of proteins defines a subset of factors that physically associate
and function to maintain the positional identity of cells from the embryo to adult stages. PcG …
and function to maintain the positional identity of cells from the embryo to adult stages. PcG …
[HTML][HTML] EED-targeted PROTACs degrade EED, EZH2, and SUZ12 in the PRC2 complex
Deregulation of the PRC2 complex, comprised of the core subunits EZH2, SUZ12, and EED,
drives aberrant hypermethylation of H3K27 and tumorigenicity of many cancers. Although …
drives aberrant hypermethylation of H3K27 and tumorigenicity of many cancers. Although …
Targeting Polycomb systems to regulate gene expression: modifications to a complex story
Polycomb group proteins are transcriptional repressors that are essential for normal gene
regulation during development. Recent studies suggest that Polycomb repressive …
regulation during development. Recent studies suggest that Polycomb repressive …
GATA transcription factors in development and disease
M Tremblay, O Sanchez-Ferras, M Bouchard - Development, 2018 - journals.biologists.com
The GATA family of transcription factors is of crucial importance during embryonic
development, playing complex and widespread roles in cell fate decisions and tissue …
development, playing complex and widespread roles in cell fate decisions and tissue …
Design and synthesis of EZH2-based PROTACs to degrade the PRC2 complex for targeting the noncatalytic activity of EZH2
Z Liu, X Hu, Q Wang, X Wu, Q Zhang… - Journal of medicinal …, 2021 - ACS Publications
EZH2 mediates both PRC2-dependent gene silencing via catalyzing H3K27me3 and PRC2-
independent transcriptional activation in various cancers. Given its oncogenic role in …
independent transcriptional activation in various cancers. Given its oncogenic role in …
Dynamic control of enhancer repertoires drives lineage and stage-specific transcription during hematopoiesis
Enhancers are the primary determinants of cell identity, but the regulatory components
controlling enhancer turnover during lineage commitment remain largely unknown. Here we …
controlling enhancer turnover during lineage commitment remain largely unknown. Here we …