Figure 2. Effector sites of epigenetic regulator drugs.

Upregulation of DNMTs and HDACS alter gene transcription leading to human cancers including hematological malignancies. Similarly, loss of TET supporting proteins leads to decreased gene transcription. DNMT, IDH1, and IDH2 inhibitors inhibit DNA methylation pathways to mitigate loss of function, gene down regulation from methylation. Other epigenetic regulators function through histone modifications that can lead to abnormal chromatin compaction. These include HDACs which reduce acetylation and histone methyl transferases (HMTs) which promote histone methylation. EZH2 inhibitors target the EZH2 HMT to reduce histone methylation to correct gene dysregulation. Adapted with permission from¹⁰³.