Histone Methyltransferase DOT1L as a Promising Epigenetic Target for Treatment of Solid Tumors.

ABSTRACT: The histone lysine methyltransferase DOT1L (DOT1-like histone lysine methyltransferase) is responsible for the epigenetic regulation of gene expression through specific methylation of lysine79 residue of histone H3 (H3K79) in actively transcribed genes. Its normal activity is crucial for embryonic development and adult tissues functions, whereas its aberrant functioning is known to contribute to leukemogenesis. DOT1L is the only lysine methyltransferase that does not contain a SET domain, which is a feature that allowed the development of selective DOT1L inhibitors that are currently investigated in Phase I clinical trials for cancer treatment. Recently, abnormal expression of this enzyme has been associated with poor survival and increased aggressiveness of several solid tumors. In this r

SUBMITTER: Alexandrova E 

PROVIDER: S-EPMC9043692 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature