Semi-quantitative mass spectrometry in AML cells identifies new non-genomic targets of the EZH2 methyltransferase
Alterations to the gene encoding the EZH2 (KMT6A) methyltransferase, including both gain-
of-function and loss-of-function, have been linked to a variety of haematological …
of-function and loss-of-function, have been linked to a variety of haematological …
Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia
Enhancer of zeste homolog 2 (EZH2) and related EZH1 control gene expression and
promote tumorigenesis via methylating histone H3 at lysine 27 (H3K27). These …
promote tumorigenesis via methylating histone H3 at lysine 27 (H3K27). These …
Preclinical characterization of E7438, a potent, selective EZH2 inhibitor with robust antitumor activity against EZH2 mutated NHL xenografts in mice
H Keilhack - Annals of Oncology, 2013 - annalsofoncology.org
The coupled enzymatic activity of wild-type and mutant EZH2 results in hyper-trimethylation
of histone H3 lysine 27 (H3K27), which drives lymphomagenesis in heterozygous patients …
of histone H3 lysine 27 (H3K27), which drives lymphomagenesis in heterozygous patients …
Preclinical characterization of E7438, a potent, selective inhibitor of protein methyltransferase EZH2 with robust antitumor activity against EZH2 mutated non-Hodgkin …
Abstract 3712 The coupled enzymatic activity of wild-type and mutant EZH2 results in hyper-
trimethylation of histone H3 lysine 27 (H3K27), which drives lymphomagenesis in …
trimethylation of histone H3 lysine 27 (H3K27), which drives lymphomagenesis in …
Dual inhibition of EZH2 and G9A/GLP histone methyltransferases by HKMTI-1-005 promotes differentiation of acute myeloid leukemia cells
All-trans-retinoic acid (ATRA)-based differentiation therapy of acute promyelocytic leukemia
(APL) represents one of the most clinically effective examples of precision medicine and the …
(APL) represents one of the most clinically effective examples of precision medicine and the …
Ectopic expression of the histone methyltransferase Ezh2 in haematopoietic stem cells causes myeloproliferative disease
A Herrera-Merchan, L Arranz, JM Ligos… - Nature …, 2012 - nature.com
Recent evidence shows increased and decreased expression of Ezh2 in cancer, suggesting
a dual role as an oncogene or tumour suppressor. To investigate the mechanism by which …
a dual role as an oncogene or tumour suppressor. To investigate the mechanism by which …
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 …
An orally bioavailable chemical probe of the lysine methyltransferases EZH2 and EZH1
EZH2 or EZH1 is the catalytic subunit of the polycomb repressive complex 2 that catalyzes
methylation of histone H3 lysine 27 (H3K27). The trimethylation of H3K27 (H3K27me3) is a …
methylation of histone H3 lysine 27 (H3K27). The trimethylation of H3K27 (H3K27me3) is a …
The pleiotropic roles of EZH2 in T-cell immunity and immunotherapy
Y Wang, T Bui, Y Zhang - International Journal of Hematology, 2022 - Springer
EZH2 is a histone methyltransferase. It catalyzes trimethylation of histone H3 at lysine 27
(H3K27me3) to control gene transcription critical for cell proliferation, differentiation …
(H3K27me3) to control gene transcription critical for cell proliferation, differentiation …