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  Discovery of selective aminothiazole aurora kinase inhibitors

Andersen, C. B., Wan, Y., Chang, J. W., Riggs, B., Lee, C., Liu, Y., et al. (2008). Discovery of selective aminothiazole aurora kinase inhibitors. ACS CHEMICAL BIOLOGY, 3(3), 180-192. doi:10.1021/cb700200w.

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Datensatz-Permalink: https://hdl.handle.net/11858/00-001M-0000-0015-3AF2-F Versions-Permalink: https://hdl.handle.net/11858/00-001M-0000-0015-4EAE-4
Genre: Zeitschriftenartikel

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 Urheber:
Andersen, Carsten B.1, Autor
Wan, Yongqin1, Autor
Chang, Jae W.2, Autor
Riggs, Blake3, Autor
Lee, Christian1, Autor
Liu, Yi1, Autor
Sessa, Fabio4, Autor
Villa, Fabrizio4, Autor
Kwiatkowski, Nicholas2, Autor
Suzuki, Melissa5, Autor
Nallan, Laxman1, Autor
Heald, Rebecca3, Autor
Musacchio, Andrea6, Autor           
Gray, Nathanael S.2, Autor
Affiliations:
1Department of Biological Chemistry, Genomics Institute of the Novartis Research Foundation, 10675 John Jay Hopkins Drive, San Diego, California 92121, ou_persistent22              
2Department of Cancer Biology, Dana Farber Cancer Institute, Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, 250 Longwood Avenue, Boston, Massachusetts 02115, ou_persistent22              
3Department of Molecular and Cell Biology, University of California, Berkeley, California 94720, ou_persistent22              
4Department of Experimental Oncology, European Institute of Oncology, Via Adamello, 16-20139 Milan, Italy, ou_persistent22              
5Invitrogen Corporation, Madison, Wisconsin 53558, ou_persistent22              
6Abt. I:Mechanistische Zellbiologie, Max Planck Institute of Molecular Physiology, Max Planck Society, ou_1753287              

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 Zusammenfassung: 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.

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 Datum: 2008
 Publikationsstatus: Erschienen
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 Ort, Verlag, Ausgabe: -
 Inhaltsverzeichnis: -
 Art der Begutachtung: -
 Identifikatoren: ISI: 000254218800007
DOI: 10.1021/cb700200w
 Art des Abschluß: -

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Titel: ACS CHEMICAL BIOLOGY
Genre der Quelle: Zeitschrift
 Urheber:
Affiliations:
Ort, Verlag, Ausgabe: -
Seiten: - Band / Heft: 3 (3) Artikelnummer: - Start- / Endseite: 180 - 192 Identifikator: ISSN: 1554-8929