VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo
| Autor: | Golec Julian M C, Richele K Rasmussen, Cecile Demur, Michael Su, Tomoko Nakayama, Abi O Ajose-Adeogun, Karen Miller, David Bebbington, Elizabeth A Harrington, Thierry Hercend, Anita Diu-Hercend, Jeff Moore, Joanne A Graham |
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| Rok vydání: | 2003 |
| Předmět: |
Aurora A kinase
Aurora inhibitor Mice Nude Apoptosis Biology Protein Serine-Threonine Kinases Bioinformatics General Biochemistry Genetics and Molecular Biology Piperazines Histones chemistry.chemical_compound Mice Aurora kinase Aurora Kinases Cell Line Tumor Neoplasms Animals Humans Danusertib Enzyme Inhibitors VX-680 Molecular Structure Cell Cycle General Medicine ZM447439 Rats chemistry Cancer research Aurora Kinase C Aurora Kinase B Female |
| Zdroj: | Nature medicine. 10(3) |
| ISSN: | 1078-8956 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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