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Anti-Cancer Effects of CKD-581, a Potent Histone Deacetylase Inhibitor against Diffuse Large B-Cell Lymphoma
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Kim, Soo Jin | - |
dc.contributor.author | Kim, U. Ji | - |
dc.contributor.author | Yoo, Hae Yong | - |
dc.contributor.author | Choi, Yong June | - |
dc.contributor.author | Kang, Keon Wook | - |
dc.date.accessioned | 2023-04-19T00:32:49Z | - |
dc.date.available | 2023-04-19T00:32:49Z | - |
dc.date.created | 2020-08-10 | - |
dc.date.created | 2020-08-10 | - |
dc.date.issued | 2020-06 | - |
dc.identifier.citation | International Journal of Molecular Sciences, Vol.21 No.12, pp.4377-12 | - |
dc.identifier.issn | 1661-6596 | - |
dc.identifier.uri | https://hdl.handle.net/10371/190307 | - |
dc.description.abstract | Double-hit lymphoma (DHL) and double-expressor lymphoma (DEL) are aggressive forms of lymphoma that require better treatments to improve patient outcomes. CKD-581 is a new histone deacetylase (HDAC) inhibitor that exhibited a better safety profile in clinical trials compared to other HDAC inhibitors. Here, we demonstrate that CKD-581 inhibited the class I-II HDAC family via histone H3 and tubulin acetylation. CKD-581 treatment also up-regulated the phosphorylation of histone H2AX (gamma H2AX, DNA double-strand break marker), and reduced levels of MYC and anti-apoptotic proteins such as BCL-2, BCL-6, BCL-L-X, and MCL-1 in DH/DE-diffuse large B cell lymphoma (DLBCL) cell lines. Ultimately, CKD-581 also induced apoptosis via poly(ADP ribose) polymerase 1 (PARP1) cleavage. In a DLBCL SCID mouse xenograft model, CKD-581 exhibited anti-cancer effects comparable with those of rituximab (CD20 mAb). Our findings suggest that CKD-581 could be a good candidate for the treatment of DLBCL. | - |
dc.language | 영어 | - |
dc.publisher | Multidisciplinary Digital Publishing Institute (MDPI) | - |
dc.title | Anti-Cancer Effects of CKD-581, a Potent Histone Deacetylase Inhibitor against Diffuse Large B-Cell Lymphoma | - |
dc.type | Article | - |
dc.identifier.doi | 10.3390/ijms21124377 | - |
dc.citation.journaltitle | International Journal of Molecular Sciences | - |
dc.identifier.wosid | 000549439900001 | - |
dc.identifier.scopusid | 2-s2.0-85087034649 | - |
dc.citation.endpage | 12 | - |
dc.citation.number | 12 | - |
dc.citation.startpage | 4377 | - |
dc.citation.volume | 21 | - |
dc.description.isOpenAccess | Y | - |
dc.contributor.affiliatedAuthor | Kang, Keon Wook | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.subject.keywordPlus | ORAL VORINOSTAT | - |
dc.subject.keywordPlus | DES-LYMPHOMES | - |
dc.subject.keywordPlus | DOUBLE-HIT | - |
dc.subject.keywordPlus | MYC | - |
dc.subject.keywordPlus | EXPRESSION | - |
dc.subject.keywordPlus | TRIAL | - |
dc.subject.keywordPlus | CHOP | - |
dc.subject.keywordPlus | MECHANISMS | - |
dc.subject.keywordPlus | RESPONSES | - |
dc.subject.keywordPlus | PATHWAYS | - |
dc.subject.keywordAuthor | CKD-581 | - |
dc.subject.keywordAuthor | diffuse large B cell lymphoma | - |
dc.subject.keywordAuthor | histone deacetylase inhibitor | - |
dc.subject.keywordAuthor | MYC | - |
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