Ferguson, Fleur M. Doctor, Zainab M. Chaikuad, Apirat Sim, Taebo Kim, Nam Doo Knapp, Stefan Gray, Nathanael S. 2024-01-20T00:32:40Z 2024-01-20T00:32:40Z 2021-09-05 2017-09-15 0960-894X https://pubs.kist.re.kr/handle/201004/122278 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. (C) 2017 Elsevier Ltd. All rights reserved. English Pergamon Press Ltd. CHROMOSOMAL PASSENGER COMPLEX BARASERTIB AZD1152 ERK5 MAPK7 OVEREXPRESSION ANEUPLOIDY EFFICACY SAFETY Characterization of a highly selective inhibitor of the Aurora kinases Article 10.1016/j.bmcl.2017.08.016 1 Bioorganic & Medicinal Chemistry Letters, v.27, no.18, pp.4405 - 4408 Bioorganic & Medicinal Chemistry Letters 27 18 4405 4408 scie scopus 000410730200031 2-s2.0-85028763688 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article CHROMOSOMAL PASSENGER COMPLEX BARASERTIB AZD1152 ERK5 MAPK7 OVEREXPRESSION ANEUPLOIDY EFFICACY SAFETY Aurora kinase Selective kinase inhibitor Pan-Aurora inhibitor Mitosis Cancer