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题名: Drug-mediated inhibition of Fli-1 for the treatment of leukemia
作者: Li, Y-J; Zhao, X.; Vecchiarelli-Federico, L. M.1; Li, Y.; Datti, A.2, 3; Cheng, Y.4; Ben-David, Y.1
刊名: BLOOD CANCER JOURNAL
关键词: erythroleukemia ; Fli-1 ; drug inhibition
英文摘要: The Ets transcription factor, Fli-1 is activated in murine erythroleukemia and overexpressed in various human malignancies including Ewing's sarcoma, induced by the oncogenic fusion protein EWS/Fli-1. Recent studies by our group and others have demonstrated that Fli-1 plays a key role in tumorigenesis, and disrupting its oncogenic function may serve as a potential treatment option for malignancies associated with its overexpression. Herein, we describe the discovery of 30 anti-Fli-1 compounds, characterized into six functional groups. Treatment of murine and human leukemic cell lines with select compounds inhibits Fli-1 protein or mRNA expression, resulting in proliferation arrest and apoptosis. This anti-cancer effect was mediated, at least in part through direct inhibition of Fli-1 function, as anti-Fli-1 drug treatment inhibited Fli-1 DNA binding to target genes, such as SHIP-1 and gata-1, governing hematopoietic differentiation and proliferation. Furthermore, treatment with select Fli-1 inhibitors revealed a positive relationship between the loss of DNA-binding activity and Fli-1 phosphorylation. Accordingly, anti-Fli-1 drug treatment significantly inhibited leukemogenesis in a murine erythroleukemia model overexpressing Fli-1. This study demonstrates the ability of this drug-screening strategy to isolate effective anti-Fli-1 inhibitors and highlights their potential use for the treatment of malignancies overexpressing this oncogene.
出版日期: 2012
卷号: 2, 页码:e54
DOI标识: 10.1038/bcj.2011.52
语种: 英语
ISSN号: 2044-5385
资助信息: Ontario Institute for Cancer Research (OICR); Canadian Institute of Health Research (CIHR)[MOP-110952]
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/10393
Appears in Collections:植物化学与西部植物资源持续利用国家重点实验室_期刊论文

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作者单位: 1.Univ Toronto, Dept Med Biophys, Sunnybrook Hlth Sci Ctr, Toronto, ON M4N 3M5, Canada
2.Mt Sinai Hosp, Samuel Lunenfeld Res Inst, SMART Facil, Toronto, ON M5G 1X5, Canada
3.Univ Perugia, Dept Expt Med & Biochem Sci, I-06100 Perugia, Italy
4.Chinese Acad Sci, Kunming Inst Bot, Kunming, Peoples R China

Recommended Citation:
Li, YJ; Zhao, X; Vecchiarelli-Federico, LM; Li, Y; Datti, A; Cheng, Y; Ben-David, Y.Drug-mediated inhibition of Fli-1 for the treatment of leukemia,BLOOD CANCER JOURNAL,2012,2():e54
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