Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 권종범 | * |
dc.date.accessioned | 2020-12-07T16:30:02Z | - |
dc.date.available | 2020-12-07T16:30:02Z | - |
dc.date.issued | 2020 | * |
dc.identifier.issn | 2045-2322 | * |
dc.identifier.other | OAK-28159 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/255613 | - |
dc.description.abstract | Bromodomain (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. © 2020, The Author(s). | * |
dc.language | English | * |
dc.publisher | Nature Research | * |
dc.title | Cytotoxic activity of bromodomain inhibitor NVS-CECR2-1 on human cancer cells | * |
dc.type | Article | * |
dc.relation.issue | 1 | * |
dc.relation.volume | 10 | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.journaltitle | Scientific Reports | * |
dc.identifier.doi | 10.1038/s41598-020-73500-7 | * |
dc.identifier.wosid | WOS:000577143400093 | * |
dc.identifier.scopusid | 2-s2.0-85091764958 | * |
dc.author.google | Park S.G. | * |
dc.author.google | Lee D. | * |
dc.author.google | Seo H.-R. | * |
dc.author.google | Lee S.-A. | * |
dc.author.google | Kwon J. | * |
dc.contributor.scopusid | 권종범(7202469069) | * |
dc.date.modifydate | 20240422113429 | * |