EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations

By M. McCabe, H. Ott, G. Ganji, S. Korenchuk, Christine Thompson, G. V. Aller, Yan Liu, A. P. Graves, A. Pietra, Elsie Diaz and 12 more. Nature, 2012

1,719 citations recorded by the source corpus.

Subfields: Molecular Biology

View Paper: https://www.semanticscholar.org/paper/7b95206c4c380b9af7020c4551d5feccc418f695

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Citations in the corpus

EZH2 is required for germinal center formation and somatic EZH2 mutations promote lymphoid transformation (2013, background): “We and others have noted that H3K27 ChIP-seq profiles as well as gene expression profiles induced by EZH2 inhibitors are variable between cell lines (McCabe et al., 2012b), suggesting that hyperactive EZH2 molecule might lead to epigenetic instability and stochastic aberrant epigenetic 3…”
Occupying chromatin: Polycomb mechanisms for getting to genomic targets, stopping transcriptional traffic, and staying put (2013, background): “Recently, analyses of leukemia patients have supplied the first examples of oncogenic missense mutations in PcG genes (McCabe et al., 2012a; Sneeringer et al., 2010).”
Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2 (2013, result): “are similar to those of other published EZH2 inhibitors (6, 7).”
PD-L1 (B7-H1) and PD-1 Pathway Blockade for Cancer Therapy: Mechanisms, Response Biomarkers and Combinations (2016, background): “In support of this, treatment with cancer epigenetic reprogramming drugs including EZH2 inhibitors, DZNep (103) (a selective inhibitor of EZH2methyltransferase activity), GSK126 (104), and 5-aza-2′deoxycytidine (5-AZA dC) (a DNMT inhibitor) enhances tumor TH1-chemokine production and T cell traffick”
Metabolic reprogramming and epigenetic modifications on the path to cancer (2021, background): “H3K27 methyltransferase EZH2 is the catalytic component of PRC2, an established transcriptional repressor (Cao et al., 2002; Levine et al., 2004).”
The histone methyltransferase SMYD2 methylates PARP1 and promotes poly(ADP-ribosyl)ation activity in cancer cells. (2014, background): “and inhibitors targeting some histone methyltransferases including SMYD2 have already been reported as candidates of anticancer drugs [32,49,50].”
Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders (2014, background): “Clinical and molecular characterization of a rare syndrome of acute promyelocytic leukemia associated with translocation (11;17).”
Oncogenic histone methyltransferase EZH2: A novel prognostic marker with therapeutic potential in endometrial cancer (2017, positive): “GSK126, an EZH2 inhibitor, markedly suppresses the growth of several types of cancer, including B-cell lymphoma [17].”