title: S39, a novel Aurora B kinase inhibitor, shows potent antineoplastic activity in human Hela cervical cancer cell line.
abstract: Aurora kinases, frequently detected to be over-expressing in human tumors, regulate many essential events during mitosis progression and have been regarded as potentially important targets for cancer therapy. S39 is a novel potent inhibitor of Aurora B kinase with the IC50 90.07 nM in the biochemical assay in an ATP competitive manner. S39 treatment on human tumor cells can inhibit the phosphorylation of Histone H3 (Ser10), a direct downstream substrate of Aurora B kinase, indicating S39 inhibits endogenous Aurora B kinase activity in cell-based level. Furthermore, S39 treatment blocks cell proliferation, inhibits colony formation and induces apoptosis in a wide range of human tumor cell lines. These results indicate that S39 is a potential lead compound to be an Aurora B inhibitor.
authors: Institute of Genetics, School of Life Science, Fudan University, Shanghai, 200433, People's Republic of China. lijiejocelin@gmail.com
authors: Jie
authors: J
authors: Li
authors: Qingyu
authors: Q
authors: Lang
authors: Haoxing
authors: H
authors: Zhang
authors: Qiang
authors: Q
authors: Huang
authors: Long
authors: L
authors: Yu
mesh_terms: D000970:Antineoplastic Agents / Q000302:isolation & purification* / Q000378:metabolism*; D017209:Apoptosis; D064107:Aurora Kinase B / Q000037:antagonists & inhibitors*; D049109:Cell Proliferation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000302:isolation & purification* / Q000378:metabolism*; D004847:Epithelial Cells / Q000187:drug effects* / Q000502:physiology*; D005260:Female; D006367:HeLa Cells; D006657:Histones / Q000378:metabolism; D006801:Humans; D020128:Inhibitory Concentration 50; D010766:Phosphorylation / Q000187:drug effects; D011499:Protein Processing, Post-Translational / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D006657:Histones; C576921:AURKB protein, human; D064107:Aurora Kinase B