[Comment] Targeting EZH2 with tazemetostat

Enhancer of zeste homolog 2 (EZH2) is a subunit of the chromatin remodelling polycomb repressive complex 2. EZH2 is a histone methyltransferase and trimethylates histone H3 lysine 27 (H3K27). EZH2 activation contributes to epigenetic transcriptional silencing because H3K27 methylation is a repressive histone modification.1 Physiologically, EZH2 activity is high in stem or progenitor cells, in which EZH2 represses genes associated with cell cycle arrest and promotes self-renewal. However, in differentiated cells EZH2 activity is opposed by the switch/sucrose non-fermentable (SWI/SNF) multiprotein complex, which promotes terminal differentiation and regulates self-renewal.
Source: The Lancet Oncology - Category: Cancer & Oncology Authors: Tags: Comment Source Type: research