DZNep may directly target putative cancer stem cells in biliary tract cancer cells by inhibition of PRC2

Introduction: The Polycomb Repressive Complex 2 (PRC2) silences genes via trimethylation of histone 3 at lysine 27 (H3K27me3). This type of epigenetic silencing represents one mechanism of malignant cells to gain and maintain stem cell-like status. It was shown that 3-Deazaneplanocin-A (DZNep), an S-adenosyl-L-homocysteine hydrolase inhibitor, is able to disturb the PRC2 complex and to reduce H3K27me mediated gene silencing.