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YD277 Suppresses Triple-Negative Breast Cancer Partially Through Activating the Endoplasmic Reticulum Stress Pathway

zhpd55 添加于 2017/8/16 15:56:03  1016次阅读 | 0次推荐 | 0个评论

Triple-negative breast cancer (TNBC) is an aggressive malignancy with poor clinical outcomes. YD277 is a novel small molecule derived from ML264, a KLF5 inhibitor that elicits cytotoxic effects in colon cancer cell lines. Our previous studies suggest that Krüpple-like factor 5 (KLF5) is a promising therapeutic target for TNBC. In this study, we demonstrated that YD277 significantly induced G1 cell cycle arrest and apoptosis in MDA-MB-231 and MDA-MB-468 TNBC cells, independent of KLF5 inhibition. YD277 also reduced the protein expression levels of Cyclin D1, Bcl2 and Bclxl and promoted the expression of p21 and p27. Moreover, the pro-apoptotic activity of YD277 in TNBC was mediated by the transcription of IRE1α, a key molecule in the endoplasmic reticulum (ER) stress pathway. Finally, YD277 (15 mg/kg) significantly suppressed the growth of MDA-MB-231 tumor xenografts in nude mice. These findings indicate that YD277 is a promising chemotherapeutic candidate for TNBC.

作 者:Zekun Chen, Qiuju Wu, Ye Ding, Wenhui Zhou, Rong Liu, Haiying Chen, Jia Zhou, Jing Feng, Ceshi Chen
期刊名称: Theranostics
期卷页: June 11, 2017 第7卷 第8期 2339-2349页
学科领域:医学科学 » 药物学 » 特种药物
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原文链接:http://www.thno.org/v07p2339.htm
DOI: 10.7150/thno.17555
ISBN:
关键词: YD277, KLF5, Triple-Negative Breast Cancer, IRE1α, ER stress
全文地址: 下载
备 注: Breast cancer is one of the most commonly diagnosed cancers and the second leading cause of cancer-related mortality in women. Indeed, breast cancer alone accounts for 29% of all new cancer cases in women [1]. Triple-negative breast cancer (TNBC) is a breast cancer subtype that lacks estrogen receptor (ERα), progesterone receptor (PR) and human epidermal growth factor receptor 2 (HER2) expression, and it accounts for 10-24% of invasive breast cancer cases. Compared to patients with other breast cancer subtypes, TNBC patients are usually younger and have poorer survival regardless of tumor stage [2]. Traditional targeted therapies have little success or even fail to benefit TNBC patients [3]. Given the lack of effective targeted therapeutics for TNBC patients, the development of new treatment regimens is urgently needed.
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