EZH2 inhibitors are small molecules designed to specifically inhibit the enzymatic activity of EZH2, thereby preventing the methylation of H3K27. By blocking this methylation, EZH2 inhibitors can reactivate silenced tumor suppressor genes and disrupt cancer cell proliferation. Some of the well-known EZH2 inhibitors include tazemetostat, GSK126, and CPI-1205.
