Tag: EZH2

DM-01 is a Powerful and Selective EZH2 Inhibitor

Enhancer of zeste homolog 2 (EZH2) is a histone methyltransferase and a catalytic component of polycomb repressive complex 2 (PRC2). EZH2 catalyzes tri-methylation of histone H3 at Lys 27 (H3K27me3) to regulate gene expression through epigenetic machinery. In addition, EZH2 also functions both as a transcriptional suppressor and a...

PF-06821497 is an Oral Active Inhibitor of Enhancer of Zeste Homolog 2 (EZH2)

Epigenetic alterations are a recognized hallmark of cancer cells, and several lines of evidence link aberrant EZH2 (Enhancer of Zeste Homolog 2) activity to tumor initiation and progression. EZH2 is also overexpressed in multiple solid tumors and hematological malignancies, and elevated expression is often correlated with disease progression and...