Characterization of a highly selective inhibitor of the Aurora kinases

Title
Characterization of a highly selective inhibitor of the Aurora kinases
Authors
심태보Fleur M. FergusonZainab M. DoctorApirat ChaikuadNam Doo KimStefan KnappNathanael S. Gray
Keywords
Aurora kinase; Selective kinase inhibitor; Pan-Aurora inhibitor; Mitosis; Cancer
Issue Date
2017-09
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 27, NO 18-4408
Abstract
Aurora kinases play an essential role in mitosis and cell cycle regulation. In recent years Aurora kinases have proved popular cancer targets and many inhibitors have been developed. The majority of these clinical candidates are multi-targeted, rendering them inappropriate as tools for studying Aurora kinase mediated signaling. Here we report discovery of a highly selective inhibitor of Aurora kinases A, B and C, with potent cellular activity and minimal off-target activity (PLK4). The X-ray co-crystal structure of Aurora A in complex with compound 2 is reported, and provides insights into the structural determinants of ligand binding and selectivity.
URI
http://pubs.kist.re.kr/handle/201004/67090
ISSN
0960-894X
Appears in Collections:
KIST Publication > Article
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