EZH2 depletion potentiates MYC degradation inhibiting neuroblastoma and small cell carcinoma tumor formation
L Wang, C Chen, Z Song, H Wang, M Ye… - Nature …, 2022 - nature.com
Efforts to therapeutically target EZH2 have generally focused on inhibition of its
methyltransferase activity, although it remains less clear whether this is the central …
methyltransferase activity, although it remains less clear whether this is the central …
Prolonged Ezh2 depletion in glioblastoma causes a robust switch in cell fate resulting in tumor progression
EZH2 is frequently overexpressed in glioblastoma (GBM), suggesting an oncogenic function
that could be a target for therapeutic intervention. However, reduced EZH2 activity can also …
that could be a target for therapeutic intervention. However, reduced EZH2 activity can also …
EZH2 noncanonically binds cMyc and p300 through a cryptic transactivation domain to mediate gene activation and promote oncogenesis
Canonically, EZH2 serves as the catalytic subunit of PRC2, which mediates H3K27me3
deposition and transcriptional repression. Here, we report that in acute leukaemias, EZH2 …
deposition and transcriptional repression. Here, we report that in acute leukaemias, EZH2 …
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 …
Oncogenic deregulation of EZH2 as an opportunity for targeted therapy in lung cancer
As a master regulator of chromatin function, the lysine methyltransferase EZH2 orchestrates
transcriptional silencing of developmental gene networks. Overexpression of EZH2 is …
transcriptional silencing of developmental gene networks. Overexpression of EZH2 is …
[HTML][HTML] Acquisition of a single EZH2 D1 domain mutation confers acquired resistance to EZH2-targeted inhibitors
Although targeted therapies have revolutionized cancer treatment, overcoming acquired
resistance remains a major clinical challenge. EZH2 inhibitors (EZH2i), EPZ-6438 and …
resistance remains a major clinical challenge. EZH2 inhibitors (EZH2i), EPZ-6438 and …
A covalently bound inhibitor triggers EZH 2 degradation through CHIP‐mediated ubiquitination
X Wang, W Cao, J Zhang, M Yan, Q Xu, X Wu… - The EMBO …, 2017 - embopress.org
Enhancer of zeste homolog 2 (EZH 2) has been characterized as a critical oncogene and a
promising drug target in human malignant tumors. The current EZH 2 inhibitors strongly …
promising drug target in human malignant tumors. The current EZH 2 inhibitors strongly …
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 …
EZH2 as a potential target in cancer therapy
MT McCabe, CL Creasy - Epigenomics, 2014 - Taylor & Francis
Over the last several years, dysregulation of epigenetic mechanisms including DNA and
histone methylation has been recognized as a hallmark of cancer. Alterations of epigenetic …
histone methylation has been recognized as a hallmark of cancer. Alterations of epigenetic …
Roles of the EZH2 histone methyltransferase in cancer epigenetics
JA Simon, CA Lange - Mutation Research/Fundamental and Molecular …, 2008 - Elsevier
EZH2 is the catalytic subunit of Polycomb repressive complex 2 (PRC2), which is a highly
conserved histone methyltransferase that targets lysine-27 of histone H3. This methylated …
conserved histone methyltransferase that targets lysine-27 of histone H3. This methylated …