ZM 447439 inhibition of aurora kinase induces Hep2 cancer cell apoptosis in three-dimensional culture

A novel compound against oncogenic Aurora kinase A overcomes imatinib resistance in chronic myeloid leukemia cells

“…Disruption of Aurora kinase activity induces abnormal spindle pole organization, centrosome separation and chromosome congression (23). Ultimately, cells treated with Aurora kinase inhibitor undergo cell growth inhibition through the development of deleterious aneuploidy (24,25). In this report, we found that AKI603 inhibited Aur-A kinase and presented anti-leukemia effects in KBM5 cells, as well as KBM5-T315I cells, suggesting a possible novel and potent target in treating imatinib-resistant CML.…”

Novel E3 ligase component FBXL7 ubiquitinates and degrades Aurora A, causing mitotic arrest

“…Due to the important role of Aurora A during mitosis, its robust expression in many types of cancer with high proliferative rates and its link to poor outcomes in patients with cancer, results of these studies suggest a potential role for Aurora A small-molecule inhibitors. [32][33][34] One advantage of using Aurora A inhibitors with chemotherapeutic agents is their selectively toward dividing cells, therefore YFP-FBXL7 (Fig. 5B).…”

Aurora kinase A inhibition-induced autophagy triggers drug resistance in breast cancer cells

“…siRNA for downregulating gene expression was done by transfection of RNA oligonucleotides with lipofectamine 2000 (Invitrogen, 11668) according to the manufacturer's instructions. The negative control (NC) siRNA and siRNAs against SQSTM1, AURKA, MAP1LC3, ATG5 and BECN1 were synthesized by Shanghai GenePharma Co. For SQSTM1, two siRNA oligonucleotides were used, SQSTM1-B: 5'-GGA CCC ATC TGT CTT CAA A-3', SQSTM1-C: 5'-GCA TTG AAG TTG ATA TCG A-3'; 41 For AURKA, two siRNA oligonucleotides were used, AURKA-1: 5'-AUG CCC UGU CUU ACU GUC A-3', 8 AURKA-2: 5'-AAC GTG TTC TCG TGA CTC AGC-3'; 51 For AURKB, 5'-AAC GCG GCA CUU CAC AAU UGA-3'; 52 For MAP1LC3, a pool of three siRNA oligonucleotides was used, Quantification of EGFP-LC3 puncta assay. Cells were transfected with EGFP-LC3 constructs (Addgene, 11546) 56 in Opti-MEM (Invitrogen, 11058) using Lipofectamine 2000 (Invitrogen, 11668).…”