gsk2879552 and Leukemia--Myeloid--Acute

Topics: Benzoates; Cyclopropanes; Humans; Leukemia, Myeloid, Acute; Lysine; Myelodysplastic Syndromes

Lysine specific demethylase 1 (LSD1) is a histone modifying enzyme that suppresses gene expression through demethylation of lysine 4 on histone H3. The anti-tumor activity of GSK2879552 and GSK-LSD1, potent, selective irreversible inactivators of LSD1, has previously been described. Inhibition of LSD1 results in a cytostatic growth inhibitory effect in a range of acute myeloid leukemia cell lines. To enhance the therapeutic potential of LSD1 inhibition in this disease setting, a combination of LSD1 inhibition and all-

Topics: Antineoplastic Agents; Apoptosis; Benzoates; Caspases; Cell Differentiation; Cell Line, Tumor; Cell Proliferation; Cyclopropanes; Dose-Response Relationship, Drug; Drug Synergism; Gene Expression Profiling; Gene Expression Regulation, Neoplastic; Histone Demethylases; Humans; Leukemia, Myeloid, Acute; Treatment Outcome; Tretinoin

LSD1 is implicated in a number of malignancies and has emerged as an exciting target. As part of our sustained efforts to develop novel reversible LSD1 inhibitors for epigenetic therapy of cancers, in this study, we reported a series of stilbene derivatives and evaluated their LSD1 inhibitory activities, obtaining several compounds as potent LSD1 inhibitors with IC

Topics: Antineoplastic Agents; Cell Proliferation; Cell Survival; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; Enzyme Inhibitors; Histone Demethylases; Humans; Leukemia, Myeloid, Acute; Molecular Docking Simulation; Molecular Structure; Stilbenes; Structure-Activity Relationship; THP-1 Cells