DOT1L (DOT1 like histone H3K79 methyltransferase)

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Title: DOT1L (DOT1 like histone H3K79 methyltransferase)
Author: Bernt, Kathrin M; Neff, Tobias
Abstract: DOT1L is a histone lysine methyltransferase (KMT). It is the only known methyltransferase for lysine residue 79 on histone 3 (H3K79). The active site of DOT1L bears more homology to the active site in Protein Arginin Methyl Transferases (PRMTs) than the SET domain of other KMTs. DOT1L has important roles in normal development and cellular differentiation. DOT1L plays especially important roles in normal hematopoiesis and in leukemia. Initially characterized as a therapeutic target in MLL-rearranged acute leukemias, recent data suggest that DOT1L is also therapeutic target in other molecular subtypes of acute leukemia and in selected solid tumors. A phase 1 clinical trial of a small molecule inhibitor of Dot1L has been described, with encouraging responses being reported.
Subject: DOT1L; Epigenetics; Methyltransferase; Leukemia; Genes Section; Genes, Neoplasm; Humans; Leukemia, Lymphoid/*classification/genetics/pathology; Lymphatic Diseases/classification/genetics/pathology; Lymphocytes/pathology; Lymphoma/*classification/genetics/pathology; Oncogene Proteins, Fusion/genetics; Paraproteinemias/classification/genetics/pathology
Publisher: ARMGHM - Atlas Génétique des Cancers
Date: 2017

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