Covalent histone modifications—miswritten, misinterpreted and mis-erased in human cancers
Post-translational modification of histones provides an important regulatory platform for
processes such as gene transcription and DNA damage repair. It has become increasingly …
processes such as gene transcription and DNA damage repair. It has become increasingly …
Tumour-initiating cells: challenges and opportunities for anticancer drug discovery
BBS Zhou, H Zhang, M Damelin, KG Geles… - Nature reviews Drug …, 2009 - nature.com
The hypothesis that cancer is driven by tumour-initiating cells (popularly known as cancer
stem cells) has recently attracted a great deal of attention, owing to the promise of a novel …
stem cells) has recently attracted a great deal of attention, owing to the promise of a novel …
Discovery of a first-in-class EZH2 selective degrader
The enhancer of zeste homolog 2 (EZH2) is the main enzymatic subunit of the PRC2
complex, which catalyzes trimethylation of histone H3 lysine 27 (H3K27me3) to promote …
complex, which catalyzes trimethylation of histone H3 lysine 27 (H3K27me3) to promote …
Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation
W Qi, HM Chan, L Teng, L Li, S Chuai… - Proceedings of the …, 2012 - National Acad Sciences
Ezh2 (Enhancer of zeste homolog 2) protein is the enzymatic component of the Polycomb
repressive complex 2 (PRC2), which represses gene expression by methylating lysine 27 of …
repressive complex 2 (PRC2), which represses gene expression by methylating lysine 27 of …
Aberrations of EZH2 in Cancer
A Chase, NCP Cross - Clinical cancer research, 2011 - AACR
Control of gene expression is exerted at a number of different levels, one of which is the
accessibility of genes and their controlling elements to the transcriptional machinery …
accessibility of genes and their controlling elements to the transcriptional machinery …
Identification of potent, selective, cell-active inhibitors of the histone lysine methyltransferase EZH2
SK Verma, X Tian, LV LaFrance… - ACS medicinal …, 2012 - ACS Publications
The histone H3-lysine 27 (H3K27) methyltransferase EZH2 plays a critical role in regulating
gene expression, and its aberrant activity is linked to the onset and progression of cancer …
gene expression, and its aberrant activity is linked to the onset and progression of cancer …
Canonical Wnt signaling regulates Slug activity and links epithelial–mesenchymal transition with epigenetic Breast Cancer 1, Early Onset (BRCA1) repression
ZQ Wu, XY Li, CY Hu, M Ford… - Proceedings of the …, 2012 - National Acad Sciences
Slug (Snail2) plays critical roles in regulating the epithelial–mesenchymal transition (EMT)
programs operative during development and disease. However, the means by which Slug …
programs operative during development and disease. However, the means by which Slug …
CDK1-dependent phosphorylation of EZH2 suppresses methylation of H3K27 and promotes osteogenic differentiation of human mesenchymal stem cells
Y Wei, YH Chen, LY Li, J Lang, SP Yeh, B Shi… - Nature cell …, 2011 - nature.com
Enhancer of zeste homologue 2 (EZH2) is the catalytic subunit of Polycomb repressive
complex 2 (PRC2) and catalyses the trimethylation of histone H3 on Lys 27 (H3K27), which …
complex 2 (PRC2) and catalyses the trimethylation of histone H3 on Lys 27 (H3K27), which …
The role of EZH2 in tumour progression
Accumulated evidence shows that EZH2 is deregulated in a wide range of cancer types, and
it has a crucial role in stem cell maintenance and tumour development. Therefore, blocking …
it has a crucial role in stem cell maintenance and tumour development. Therefore, blocking …