EZH2 and neoplasm: They recently demonstrated that a gambogenic acid (GNA) derivative, GNA022, covalently binds to Cys 668 at the SET domain of EZH2 and subsequently triggers COOH terminus of Hsp70-interacting protein (CHIP)-mediated ubiquitination of EZH2, leading to promoting EZH2 degradation and inhibiting tumor growth [144].