Fig. 1

The action modes of EZH2. (1) EZH2 catalyzes H3K27me3 dependent on PCR2, which contributes to transcriptional silencing. (2) EZH2 is also capable of methylating several non-histone protein substrates (e.g. STAT3, GATA4, talin, and RORα), which contributes to both transcriptional silencing and transcriptional activation. 3) EZH2 also has a PRC2-independent role in transcriptional activation, acting as co-activator for transcription factors, such as AR-associated complex, NF-κB signaling, TCF/β-catenin and PCNA, and β-catenin and ERα