Novel orally bioavailable EZH1/2 dual inhibitors with greater antitumor efficacy than an EZH2 selective inhibitor

Polycomb repressive complex 2 ( PRC 2) methylates histone H3 lysine 27 and represses gene expression to regulate cell proliferation and differentiation. Enhancer of zeste homolog 2 ( EZH 2) or its close homolog EZH 1 functions as a catalytic subunit of PRC 2, so there are two PRC 2 complexes containing either EZH 2 or EZH 1. Tumorigenic functions of EZH 2 and its synthetic lethality with some subunits of SWI tch/Sucrose Non‐Fermentable ( SWI /...