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Novel BRD4-p53nInhibitor SDU-071 Suppresses Proliferationnand Migration of MDA-MB-231 Triple-Negative Breast Cancer Cells 新型BRD4-p53 n抑制剂SDU-071抑制MDA-MB-231三阴性乳腺癌细胞的增殖和迁移

Figshare Pub Date : 1753-01-01 DOI: 10.1021/acsptsci.4c00057.s001

Shumei Wang (167633), Kang Lei (2823794), Hsien-Tsung Lai (27660), Tingting Liu (267387), Lupei Du (1376673), Shwu-Yuan Wu (488069), Xiaohan Ye (1626769), Cheng-Ming Chiang (488070), Minyong Li (69472)

{"title":"Novel BRD4-p53nInhibitor SDU-071 Suppresses Proliferationnand Migration of MDA-MB-231 Triple-Negative Breast Cancer Cells","authors":"Shumei Wang (167633), Kang Lei (2823794), Hsien-Tsung Lai (27660), Tingting Liu (267387), Lupei Du (1376673), Shwu-Yuan Wu (488069), Xiaohan Ye (1626769), Cheng-Ming Chiang (488070), Minyong Li (69472)","doi":"10.1021/acsptsci.4c00057.s001","DOIUrl":"https://doi.org/10.1021/acsptsci.4c00057.s001","url":null,"abstract":"A promising alternative for cancer treatment involvesntargetedninhibition of the epigenetic regulator bromodomain-containing proteinn4 (BRD4); however, available BRD4 inhibitors are constrained by theirnpotency, oral bioavailability, and cytotoxicity. Herein, to overcomenthe drawback of the translational BRD4 inhibitors, we describe a novelnBRD4-p53 inhibitor, SDU-071, which suppresses BRD4 interaction withnthe p53 tumor suppressor and its biological activity in MDA-MB-231ntriple-negative breast cancer (TNBC) cells in vitro and in vivo. Thisnnovel small-molecule BRD4-p53 inhibitor suppresses cell proliferation,nmigration, and invasion by downregulating the expression of BRD4-targetedngenes, such as c-Myc and Mucin 5AC, and inducing cell cycle arrestnand apoptosis, as demonstrated in cultured MDA-MB-231 TNBC cells.nIts antitumor activity is illustrated in an orthotopic mouse xenograftnmammary tumor model. Overall, our results show that SDU-071 is a viablenoption for potentially treating TNBC as a new BRD4-p53 inhibitor.","PeriodicalId":521453,"journal":{"name":"Figshare","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"1753-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"147878735","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

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