2--hydroxychalcone and Leukemia--Myeloid--Acute

Activating mutations in FLT3 receptor tyrosine kinase are found in a third of acute myeloid leukemia (AML) patients and are associated with disease relapse and a poor prognosis. The majority of these mutations are internal tandem duplications (ITDs) in the juxtamembrane domain of FLT3, which have been validated as a therapeutic target. The clinical success of selective inhibitors targeting oncogenic FLT3, however, has been limited due to the acquisition of drug resistance. Herein the identification of a dual FLT3/microtubule polymerization inhibitor, chalcone

Topics: Antibiotics, Antineoplastic; Apoptosis; Cell Cycle Checkpoints; Cell Line, Tumor; Chalcones; Drug Resistance, Neoplasm; Enzyme Inhibitors; fms-Like Tyrosine Kinase 3; HCT116 Cells; Humans; K562 Cells; Leukemia, Myeloid, Acute; MAP Kinase Signaling System; Microtubules; Molecular Docking Simulation; Molecular Structure; Polymerization