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TY - JOUR AU - Harrington, Elizabeth A AU - Bebbington, David AU - Moore, Jeff AU - Rasmussen, Richele K AU - Ajose-Adeogun, Abi O AU - Nakayama, Tomoko AU - Graham, Joanne A AU - Demur, Cecile AU - Hercend, Thierry AU - Diu-Hercend, Anita AU - Su, Michael AU - Golec, Julian M C AU - Miller, Karen M PY - 2004 DA - 2004/03/01 TI - VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo JO - Nature Medicine SP - 262 EP - 267 VL - 10 IS - 3 AB - The Aurora kinases are essential for the regulation of chromosome segregation and cytokinesis during mitosis. Aberrant expression and activity of these kinases occur in a wide range of human tumors, and lead to aneuploidy and tumorigenesis. Here we report the discovery of a highly potent and selective small-molecule inhibitor of Aurora kinases, VX-680, that blocks cell-cycle progression and induces apoptosis in a diverse range of human tumor types. This compound causes profound inhibition of tumor growth in a variety of in vivo xenograft models, leading to regression of leukemia, colon and pancreatic tumors at well-tolerated doses. Our data indicate that Aurora kinase inhibition provides a new approach for the treatment of multiple human malignancies. SN - 1546-170X UR - https://doi.org/10.1038/nm1003 DO - 10.1038/nm1003 ID - Harrington2004 ER -