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dc.contributor.authorFerguson, Fleur M.-
dc.contributor.authorDoctor, Zainab M.-
dc.contributor.authorChaikuad, Apirat-
dc.contributor.authorSim, Taebo-
dc.contributor.authorKim, Nam Doo-
dc.contributor.authorKnapp, Stefan-
dc.contributor.authorGray, Nathanael S.-
dc.date.accessioned2024-01-20T00:32:40Z-
dc.date.available2024-01-20T00:32:40Z-
dc.date.created2021-09-05-
dc.date.issued2017-09-15-
dc.identifier.issn0960-894X-
dc.identifier.urihttps://pubs.kist.re.kr/handle/201004/122278-
dc.description.abstractAurora 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.-
dc.languageEnglish-
dc.publisherPergamon Press Ltd.-
dc.subjectCHROMOSOMAL PASSENGER COMPLEX-
dc.subjectBARASERTIB AZD1152-
dc.subjectERK5 MAPK7-
dc.subjectOVEREXPRESSION-
dc.subjectANEUPLOIDY-
dc.subjectEFFICACY-
dc.subjectSAFETY-
dc.titleCharacterization of a highly selective inhibitor of the Aurora kinases-
dc.typeArticle-
dc.identifier.doi10.1016/j.bmcl.2017.08.016-
dc.description.journalClass1-
dc.identifier.bibliographicCitationBioorganic & Medicinal Chemistry Letters, v.27, no.18, pp.4405 - 4408-
dc.citation.titleBioorganic & Medicinal Chemistry Letters-
dc.citation.volume27-
dc.citation.number18-
dc.citation.startPage4405-
dc.citation.endPage4408-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
dc.identifier.wosid000410730200031-
dc.identifier.scopusid2-s2.0-85028763688-
dc.relation.journalWebOfScienceCategoryChemistry, Medicinal-
dc.relation.journalWebOfScienceCategoryChemistry, Organic-
dc.relation.journalResearchAreaPharmacology & Pharmacy-
dc.relation.journalResearchAreaChemistry-
dc.type.docTypeArticle-
dc.subject.keywordPlusCHROMOSOMAL PASSENGER COMPLEX-
dc.subject.keywordPlusBARASERTIB AZD1152-
dc.subject.keywordPlusERK5 MAPK7-
dc.subject.keywordPlusOVEREXPRESSION-
dc.subject.keywordPlusANEUPLOIDY-
dc.subject.keywordPlusEFFICACY-
dc.subject.keywordPlusSAFETY-
dc.subject.keywordAuthorAurora kinase-
dc.subject.keywordAuthorSelective kinase inhibitor-
dc.subject.keywordAuthorPan-Aurora inhibitor-
dc.subject.keywordAuthorMitosis-
dc.subject.keywordAuthorCancer-
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