Please use this identifier to cite or link to this item: https://hdl.handle.net/11147/8927
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dc.contributor.authorDelman, Murat-
dc.contributor.authorAvcı, Sanem Tercan-
dc.contributor.authorAkçok, İsmail-
dc.contributor.authorKanbur, Tuğçe-
dc.contributor.authorErdal, Esra-
dc.contributor.authorÇağır, Ali-
dc.date.accessioned2020-07-18T08:34:08Z
dc.date.available2020-07-18T08:34:08Z
dc.date.issued2019-10
dc.identifier.issn0223-5234
dc.identifier.issn1768-3254
dc.identifier.issn0223-5234-
dc.identifier.issn1768-3254-
dc.identifier.urihttps://doi.org/10.1016/j.ejmech.2019.07.024
dc.identifier.urihttps://hdl.handle.net/11147/8927
dc.descriptionPubMed: 31306909en_US
dc.description.abstractCytotoxic effects of (R)-4'-methylklavuzon were investigated on hepatocellular carcinoma cells (HuH-7 and HepG2) and HuH-7 EpCAM(+)/CD133(+) cancer stem cells. IC50 of (R)-4'-methylklavuzon was found as 1.25 mu M for HuH-7 parental cells while it was found as 2.50 mu M for HuH-7 EpCAM(+)/CD133(+) cancer stem cells. (R)-4'-methylklavuzon tended to show more efficient in vitro cytotoxicity with its lower IC50 values on hepatocellular carcinoma cell lines compared to its lead molecule, goniothalamin and FDA-approved drugs, sorafenib and regorafenib. Cell-based Sirtuin/HDAC enzyme activity measurements revealed that endogenous Sirtuin/HDAC enzymes were reduced by 40% compared to control. SIRT1 protein levels were upregulated indicating triggered DNA repair mechanism. p53 was overexpressed in HepG2 cells. (R)-4'methylklavuzon inhibited CRM1 protein providing increased retention of p53 and RIOK2 protein in the nucleus. HuH-7 parental and EpCAM(+)/CD133(+) cancer stem cell spheroids lost intact morphology. 3D HepG2 spheroid viabilities were decreased in a correlation with upregulation in p53 protein levels. (C) 2019 Elsevier Masson SAS. All rights reserved.en_US
dc.language.isoenen_US
dc.publisherElsevier Ltd.en_US
dc.relation.ispartofEuropean Journal of Medicinal Chemistryen_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectHepatocellular carcinomaen_US
dc.subjectCancer stem cellen_US
dc.subjectSIRT1 inhibitoren_US
dc.subjectCRM1 inhibitoren_US
dc.subjectTopoisomerase I inhibitoren_US
dc.subjectKlavuzonen_US
dc.titleAntiproliferative activity of (R)-4 '-methylklavuzon on hepatocellular carcinoma cells and EpCAM(+)/CD133(+) cancer stem cells via SIRT1 and Exportin-1 (CRM1) inhibitionen_US
dc.typeArticleen_US
dc.institutionauthorDelman, Murat
dc.institutionauthorAkçok, İsmail
dc.institutionauthorKanbur, Tuğçe
dc.institutionauthorÇağır, Ali
dc.institutionauthorDelman, Murat-
dc.institutionauthorAkçok, İsmail-
dc.institutionauthorKanbur, Tuğçe-
dc.institutionauthorÇağır, Ali-
dc.departmentIzmir Institute of Technology. Chemistryen_US
dc.departmentIzmir Institute of Technology. Biotechnology and Bioengineeringen_US
dc.identifier.volume180en_US
dc.identifier.startpage224en_US
dc.identifier.endpage237en_US
dc.identifier.wosWOS:000488307100019en_US
dc.identifier.scopus2-s2.0-85068795592en_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.identifier.doi10.1016/j.ejmech.2019.07.024-
dc.identifier.pmid31306909en_US
dc.relation.doi10.1016/j.ejmech.2019.07.024en_US
dc.coverage.doi10.1016/j.ejmech.2019.07.024en_US
dc.identifier.scopusqualityQ1-
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.openairetypeArticle-
item.fulltextWith Fulltext-
item.cerifentitytypePublications-
item.grantfulltextembargo_20230101-
item.languageiso639-1en-
crisitem.author.dept04.01. Department of Chemistry-
Appears in Collections:Bioengineering / Biyomühendislik
Chemistry / Kimya
PubMed İndeksli Yayınlar Koleksiyonu / PubMed Indexed Publications Collection
Scopus İndeksli Yayınlar Koleksiyonu / Scopus Indexed Publications Collection
WoS İndeksli Yayınlar Koleksiyonu / WoS Indexed Publications Collection
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