mln-8237 and Leukemia--Monocytic--Acute

Aberrations in histone modifications are being studied in mixed-lineage leukemia (MLL)-AF9-driven acute myeloid leukemia (AML). In this study, we focused on the regulation of the differentiation of the MLL-AF9 type AML cell line THP-1. We observed that, upon phorbol 12-myristate 13-acetate (PMA) treatment, THP-1 cells differentiated into monocytes by down-regulating Aurora kinase A (AURKA), resulting in a reduction in H3S10 phosphorylation. We revealed that the AURKA inhibitor alisertib accelerates the expression of the H3K27 demethylase KDM6B, thereby dissociating AURKA and YY1 from the

Topics: Aurora Kinase A; Azepines; Benzazepines; Cell Differentiation; Chromatin Immunoprecipitation; Cyclin-Dependent Kinase Inhibitor p21; Gene Expression Regulation, Leukemic; Genes, Reporter; HEK293 Cells; Histones; Humans; Jumonji Domain-Containing Histone Demethylases; Leukemia, Monocytic, Acute; Monocytes; Myeloid-Lymphoid Leukemia Protein; Neoplasm Proteins; Oncogene Proteins, Fusion; Phosphorylation; Promoter Regions, Genetic; Protein Processing, Post-Translational; Pyrimidines; Recombinant Proteins; RNA Interference; RNA, Small Interfering; Tetradecanoylphorbol Acetate; THP-1 Cells; YY1 Transcription Factor