دورية أكاديمية
Discovery of selective aminothiazole aurora kinase inhibitors
| العنوان: | Discovery of selective aminothiazole aurora kinase inhibitors |
|---|---|
| المؤلفون: | Andersen, C., Wan, Y., Chang, J., Riggs, B., Lee, C., Liu, Y., Sessa, F., Villa, F., Kwiatkowski, N., Suzuki, M., Nallan, L., Heald, R., Musacchio, A., Gray, N. |
| المصدر: | ACS CHEMICAL BIOLOGY |
| سنة النشر: | 2008 |
| المجموعة: | Max Planck Society: MPG.PuRe |
| الوصف: | Aurora family kinases regulate important events during mitosis including centrosome maturation and separation, mitotic spindle assembly, and chromosome segregation. Misregulation of Aurora kinases due to genetic amplification and protein overexpression results in aneuploidy and may contribute to tumorigenesis. Here we report the discovery of new small molecule aminothiazole inhibitors of Aurora kinases with exceptional kinase selectivity and report a 1.7 angstrom cocrystal structure with the Aurora B:INCENP complex from Xenopus laevis. The compounds recapitulate the hallmarks of Aurora kinase inhibition, including decreased histone H3 serine 10 phosphorylation, failure to complete cytokinesis, and endoreduplication. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | unknown |
| العلاقة: | http://hdl.handle.net/11858/00-001M-0000-0015-3AF2-FTest |
| الإتاحة: | https://doi.org/10.1021/cb700200wTest http://hdl.handle.net/11858/00-001M-0000-0015-3AF2-FTest |
| رقم الانضمام: | edsbas.F6AC8B28 |
| قاعدة البيانات: | BASE |
| الوصف غير متاح. |