Characterization of a highly selective inhibitor of the Aurora kinases
DC Field | Value | Language |
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dc.contributor.author | Ferguson, Fleur M. | - |
dc.contributor.author | Doctor, Zainab M. | - |
dc.contributor.author | Chaikuad, Apirat | - |
dc.contributor.author | Sim, Taebo | - |
dc.contributor.author | Kim, Nam Doo | - |
dc.contributor.author | Knapp, Stefan | - |
dc.contributor.author | Gray, Nathanael S. | - |
dc.date.accessioned | 2021-09-03T01:44:43Z | - |
dc.date.available | 2021-09-03T01:44:43Z | - |
dc.date.created | 2021-06-19 | - |
dc.date.issued | 2017-09-15 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/82221 | - |
dc.description.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. (C) 2017 Elsevier Ltd. All rights reserved. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.subject | CHROMOSOMAL PASSENGER COMPLEX | - |
dc.subject | BARASERTIB AZD1152 | - |
dc.subject | ERK5 MAPK7 | - |
dc.subject | OVEREXPRESSION | - |
dc.subject | ANEUPLOIDY | - |
dc.subject | EFFICACY | - |
dc.subject | SAFETY | - |
dc.title | Characterization of a highly selective inhibitor of the Aurora kinases | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Sim, Taebo | - |
dc.identifier.doi | 10.1016/j.bmcl.2017.08.016 | - |
dc.identifier.scopusid | 2-s2.0-85028763688 | - |
dc.identifier.wosid | 000410730200031 | - |
dc.identifier.bibliographicCitation | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.27, no.18, pp.4405 - 4408 | - |
dc.relation.isPartOf | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.citation.title | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.citation.volume | 27 | - |
dc.citation.number | 18 | - |
dc.citation.startPage | 4405 | - |
dc.citation.endPage | 4408 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Organic | - |
dc.subject.keywordPlus | CHROMOSOMAL PASSENGER COMPLEX | - |
dc.subject.keywordPlus | BARASERTIB AZD1152 | - |
dc.subject.keywordPlus | ERK5 MAPK7 | - |
dc.subject.keywordPlus | OVEREXPRESSION | - |
dc.subject.keywordPlus | ANEUPLOIDY | - |
dc.subject.keywordPlus | EFFICACY | - |
dc.subject.keywordPlus | SAFETY | - |
dc.subject.keywordAuthor | Aurora kinase | - |
dc.subject.keywordAuthor | Selective kinase inhibitor | - |
dc.subject.keywordAuthor | Pan-Aurora inhibitor | - |
dc.subject.keywordAuthor | Mitosis | - |
dc.subject.keywordAuthor | Cancer | - |
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