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dc.contributor.author권종범-
dc.date.accessioned2020-12-07T16:30:02Z-
dc.date.available2020-12-07T16:30:02Z-
dc.date.issued2020-
dc.identifier.issn2045-2322-
dc.identifier.otherOAK-28159-
dc.identifier.urihttp://dspace.ewha.ac.kr/handle/2015.oak/255613-
dc.description.abstractBromodomain (BRD), a protein module that recognizes acetylated lysine residues on histones and other proteins, has recently emerged as a promising therapeutic target for human diseases such as cancer. While most of the studies have been focused on inhibitors against BRDs of the bromo- and extra-terminal domain (BET) family proteins, non-BET family BRD inhibitors remain largely unexplored. Here, we investigated a potential anticancer activity of the recently developed non-BET family BRD inhibitor NVS-CECR2-1 that targets the cat eye syndrome chromosome region, candidate 2 (CECR2). We show that NVS-CECR2-1 inhibits chromatin binding of CECR2 BRD and displaces CECR2 from chromatin within cells. NVS-CECR2-1 exhibits cytotoxic activity against various human cancer cells, killing SW48 colon cancer cells in particular with a submicromolar half maximum inhibition value mainly by inducing apoptosis. The sensitivity of the cancer cells to NVS-CECR2-1 is reduced by CECR2 depletion, suggesting that NVS-CECR2-1 exerts its activity by targeting CECR2. Interestingly, our data show that NVS-CECR2-1 also kills cancer cells by CECR2-independent mechanism. This study reports for the first time the cancer cell cytotoxic activity for NVS-CECR2-1 and provides a possibility of this BRD inhibitor to be developed as an anticancer therapeutic agent.-
dc.languageEnglish-
dc.publisherNATURE RESEARCH-
dc.titleCytotoxic activity of bromodomain inhibitor NVS-CECR2-1 on human cancer cells-
dc.typeArticle-
dc.relation.issue1-
dc.relation.volume10-
dc.relation.indexSCIE-
dc.relation.indexSCOPUS-
dc.relation.journaltitleSCIENTIFIC REPORTS-
dc.identifier.doi10.1038/s41598-020-73500-7-
dc.identifier.wosidWOS:000577143400093-
dc.author.googlePark, Seul Gi-
dc.author.googleLee, Daye-
dc.author.googleSeo, Hye-Ran-
dc.author.googleLee, Shin-Ai-
dc.author.googleKwon, Jongbum-
dc.contributor.scopusid권종범(7202469069)-
dc.date.modifydate20201207092343-
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자연과학대학 > 생명과학전공 > Journal papers
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