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

Sarah K. Knutson,Tim J. Wigle,Natalie Warholic,Christopher John Sneeringer,Christina J. Allain,Christine R. Klaus,Joelle D Sacks,Alejandra Raimondi,Christina R. Majer,Jeffrey Song,Margaret Porter Scott,Lei Jin,Jesse J. Smith,Edward J. Olhava,Richard Chesworth,Mikel P. Moyer,Victoria M. Richon,Robert A. Copeland,Heike Keilhack,Roy M. Pollock,Kevin Wayne Kuntz

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

2012

EZH2 is a protein methyltransferase component of the polycomb repressive complex 2 (PRC2) that installs the H3K27me3 chromatin mark. EPZ005687 inhibits EZH2 function and H3K27 trimethylation in cells and selectively kills lymphoma cells that require EZH2 for proliferation.

Keywords:

Methylation
PRC2
Molecular biology
Lymphoma
EZH2
Methyltransferase
Chromatin
Epigenetics
Cancer research
Mutant
Biology
h3k27 methylation

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