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GSK2879552 is an orally available, selective, and irreversible small molecule inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), developed by GSK. LSD1 is a histone modifying enzyme that suppresses gene expression through demethylation of lysine residues on histone H3. By inhibiting LSD1, GSK2879552 increases methylation at H3K4 and enhances the expression of tumor-suppressor genes, leading to potential antineoplastic effects. The drug has been investigated primarily for hematologic malignancies such as myelodysplastic syndromes and acute myeloid leukemia[1][3][5][6].
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