Identification of KPNB1 as a Cellular Target of Aminothiazole Derivatives with Anticancer Activity
DC Field | Value | Language |
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dc.contributor.author | Kim, Yong-Hak | - |
dc.contributor.author | Ha, Siyoung | - |
dc.contributor.author | Kim, Jungwon | - |
dc.contributor.author | Ham, Seung Wook | - |
dc.date.available | 2019-03-08T12:40:13Z | - |
dc.date.issued | 2016-07 | - |
dc.identifier.issn | 1860-7179 | - |
dc.identifier.issn | 1860-7187 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/6742 | - |
dc.description.abstract | We found that aminothiazole derivative (E)-N-(5-benzylthiazol-2-yl)-3-(furan-2-yl)acrylamide (1) has strong anticancer activity, and undertook proteomics approaches to identify the target protein of compound 1, importin1 (KPNB1). A competitive binding assay using fluorescein-labeled 1 showed that 1 has strong binding affinity for KPNB1 (K-d: approximate to 20nm). Furthermore, through western blotting assays for KPNB1, KPNA2, EGFR, ErbB2, and STAT3, we confirmed that 1 has inhibitory effects on the importin pathway. KPBN1 appears to be overexpressed in several cancer cells, and siRNA-induced inhibition of KPNB1 shows significant inhibition of cancer cell proliferation, while leaving non-cancerous cells unaffected. Therefore, compound 1 is a promising new lead for the development of KPNB1-targeted anticancer agents. Fluorescein-labeled 1 could be a useful quantitative probe for the development of novel KPNB1 inhibitors. | - |
dc.format.extent | 4 | - |
dc.language | 영어 | - |
dc.language.iso | ENG | - |
dc.publisher | WILEY-V C H VERLAG GMBH | - |
dc.title | Identification of KPNB1 as a Cellular Target of Aminothiazole Derivatives with Anticancer Activity | - |
dc.type | Article | - |
dc.identifier.doi | 10.1002/cmdc.201600159 | - |
dc.identifier.bibliographicCitation | CHEMMEDCHEM, v.11, no.13, pp 1406 - 1409 | - |
dc.description.isOpenAccess | N | - |
dc.identifier.wosid | 000380025000002 | - |
dc.identifier.scopusid | 2-s2.0-84971570010 | - |
dc.citation.endPage | 1409 | - |
dc.citation.number | 13 | - |
dc.citation.startPage | 1406 | - |
dc.citation.title | CHEMMEDCHEM | - |
dc.citation.volume | 11 | - |
dc.type.docType | Article | - |
dc.publisher.location | 독일 | - |
dc.subject.keywordAuthor | anticancer agents | - |
dc.subject.keywordAuthor | competitive binding | - |
dc.subject.keywordAuthor | KPNB1 | - |
dc.subject.keywordAuthor | LC-MS | - |
dc.subject.keywordAuthor | MS | - |
dc.subject.keywordAuthor | proteomics | - |
dc.subject.keywordPlus | SMALL-MOLECULE INHIBITOR | - |
dc.subject.keywordPlus | KINASE INHIBITORS | - |
dc.subject.keywordPlus | NUCLEAR IMPORT | - |
dc.subject.keywordPlus | CANCER | - |
dc.subject.keywordPlus | BETA | - |
dc.subject.keywordPlus | 2-AMINOTHIAZOLE | - |
dc.subject.keywordPlus | RECOGNITION | - |
dc.subject.keywordPlus | DISCOVERY | - |
dc.subject.keywordPlus | TRANSPORT | - |
dc.subject.keywordPlus | PATHWAY | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.relation.journalWebOfScienceCategory | Pharmacology & Pharmacy | - |
dc.description.journalRegisteredClass | sci | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
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