EZH2 and neoplasm: In addition to the competitive inhibitors of EZH2 expression and activity, a novel strategy to suppress EZH2 by protein degradation has been developed by Wang et al. They reported that a gambogenic acid (GNA) derivative, GNA022, specifically and covalently binds to Cys668 within the EZH2-SET domain, subsequently triggersEZH2 degradation through COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination of EZH2, enhancingEZH2 degradation and inhibiting tumor growth [98].