Intriguingly,the only FDA-approved EZH2 inhibitor, Tazemetostat, did not exhibitanti-GBM efficacy and the idea of stitching another antitumor pharmacophoreto the core structure of tazemetostat was conceived as a prudent strategyto activate its chemical architecture to exert anti-GBM effects. The gene discussed is EZH2; the disease is glioblastoma.