A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells.

By S. Knutson, T. Wigle, N. Warholic, C. Sneeringer, C. Allain, C. Klaus, Joelle D Sacks, Alejandra Raimondi, C. Majer, Jeffrey Song and 11 more. Nature Chemical Biology, 2012

770 citations recorded by the source corpus.

Subfields: Molecular Biology

View Paper: https://www.semanticscholar.org/paper/8b5632b166e98ee10052feacc5e6c1ae6645c39b

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Citations in the corpus

EZH2 is required for germinal center formation and somatic EZH2 mutations promote lymphoid transformation (2013, background): “, 2010) andmore recently through the development of highly specific and potent EZH2 small molecule inhibitors (Knutson et al., 2012; McCabe et al., 2012b; Qi et al., 2012).”
Phosphorylation of EZH2 activates STAT3 signaling via STAT3 methylation and promotes tumorigenicity of glioblastoma stem-like cells (2013, background): “Significant research efforts have been aimed at developing therapeutic agents targeted for EZH2 because highly specific EZH2 inhibitors have been reported recently (Knutson et al., 2012; McCabe et al., 2012; Qi et al., 2012).”
Occupying chromatin: Polycomb mechanisms for getting to genomic targets, stopping transcriptional traffic, and staying put (2013, background): “Recent discoveries of the first small molecule inhibitors of Polycomb machinery (Knutson et al., 2012; McCabe et al., 2012b) offer exciting new prospects for impacting PcG silencing in cancer.”
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].”
Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2 (2013, methodology): “High-throughput screening afforded a pyridone-containing EZH2 inhibitor series (5), and through iterative medicinal chemistry, we developed (N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4′-(morpholinomethyl)[1,1′-biphenyl]-3-carboxamide) (”
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).”