dot1l inhibitor

DOT1L inhibitors are a class of epigenetic modulators that target the histone methyltransferase DOT1L (Disruptor of Telomeric Silencing 1-Like). DOT1L is the sole enzyme responsible for the mono-, di-, and tri-methylation of lysine 79 on histone H3 (H3K79), a modification associated with active gene transcription. These inhibitors are primarily investigated for the treatment of MLL-rearranged (KMT2A-rearranged) leukemias, where MLL fusion proteins misdirect DOT1L to oncogenic target genes (such as HOXA9 and MEIS1), leading to their aberrant expression. Beyond leukemia, DOT1L inhibition is being explored in solid tumors, such as prostate cancer, where it may impact androgen receptor signaling and telomere integrity.

Other names

DOT1L inhibitorsDOT-1L inhibitorsDOT 1L inhibitorsdisruptor of telomeric silencing 1-like inhibitor