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 …

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 …

Activity-by-contact model of enhancer–promoter regulation from thousands of CRISPR perturbations

CP Fulco, J Nasser, TR Jones, G Munson… - Nature …, 2019 - nature.com
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 …

An androgen receptor switch underlies lineage infidelity in treatment-resistant prostate cancer

A Davies, S Nouruzi, D Ganguli, T Namekawa… - Nature cell …, 2021 - nature.com
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 …

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 …

[HTML][HTML] EED-targeted PROTACs degrade EED, EZH2, and SUZ12 in the PRC2 complex

JHR Hsu, T Rasmusson, J Robinson, F Pachl… - Cell chemical …, 2020 - cell.com
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 …

Targeting Polycomb systems to regulate gene expression: modifications to a complex story

NP Blackledge, NR Rose, RJ Klose - Nature reviews Molecular cell …, 2015 - nature.com
Polycomb group proteins are transcriptional repressors that are essential for normal gene
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 …

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 …

Dynamic control of enhancer repertoires drives lineage and stage-specific transcription during hematopoiesis

J Huang, X Liu, D Li, Z Shao, H Cao, Y Zhang… - Developmental cell, 2016 - cell.com
Enhancers are the primary determinants of cell identity, but the regulatory components
controlling enhancer turnover during lineage commitment remain largely unknown. Here we …