LSD1 inhibitors disrupt the GFI1 transcription repressor complex

Mol Cell Oncol. 2018 Aug 1;5(4):e1481813. doi: 10.1080/23723556.2018.1481813. eCollection 2018.

Abstract

Pharmacologic inhibition of KDM1A (Lysine Demethylase 1A) induces differentiation in certain subtypes of acute myeloid leukemia. Our recent studies reveal this is dependent upon drug-induced disruption of the GFI1 (Growth Factor Independent 1) transcription repressor complex, leading to activation of enhancers distributed close to genes controlling monocytic lineage differentiation.

Keywords: AML; GFI1; LSD1; acetylation; epigenetics; leukemia; methylation.