Synthesis and Biological Activity of a Cytostatic Inhibitor of MLLr Leukemia Targeting the DOT1L Protein

Synthesis and Biological Activity of a Cytostatic Inhibitor of MLLr Leukemia Targeting the DOT1L Protein

Histone methyltransferase DOT1L catalyzes mono-, di- and trimethylation of histone 3 at lysine residue 79 (H3K79) and hypermethylation of H3K79 has been linked to the development of acute leukemias characterized by the MLL (mixed-lineage leukemia) rearrangements (MLLr cells). The inhibition of H3K79...

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Bibliographic Details
Main Authors: Corentin Bon, Yang Si, Melanie Pernak, Magdalena Barbachowska, Eva Levi-Acobas, Veronique Cadet Daniel, Corinne Jallet, Dusan Ruzic, Nemanja Djokovic, Teodora Djikić, Katarina Nikolic, Ludovic Halby, Paola B. Arimondo
Format: Article
Language:English
Published: MDPI AG 2021-08-01
Series:Molecules
Subjects:
MLL rearranged leukemia
DOT1L
histone methylation
rational drug design
HMT inhibitors
bisubstrates
Online Access:https://www.mdpi.com/1420-3049/26/17/5300

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