DOT1L and cancer: Both inhibitors are of interest in some types of cancer because DOT1L is a KMT involved in abnormal methylation of H3K79 and expression of HOX genes that cause leukemia (Copeland et al., 2013), while elevated expression of the KMT, EZH2, is associated with many forms of cancer due to hypermethylation of H3K27 which facilitates transcriptional silencing (80).