YD277 Suppresses Triple-Negative Breast Cancer Partially Through Activating the Endoplasmic Reticulum Stress Pathway
文献类型：期刊论文
| 作者 | Feng J*3; Chen CS*4; Ding Y2; Zhou WH3,4; Liu R4; Chen HY2; Wu QJ1,4; Zhou J*2; Chen ZK3,4,5 |
| 刊名 | Theranostics
 |
| 出版日期 | 2017 |
| 卷号 | 7期号:8页码:2339-2349 |
| 关键词 | Er Stress Ire1α Klf5 Triple-negative Breast Cancer Yd277 |
| DOI | chenc@mail.kiz.ac.cn;fengjing8801530@163.com; jizhou@utmb.edu |
| 英文摘要 | 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. |
| 语种 | 英语 |
| 资助机构 | This work was supported by grants from "Personalized Medicines – Molecular Signature-based Drug Discovery and Development," a Strategic Priority Research Program of the Chinese Academy of Sciences (XDA12010303 to Chen, C.); The Shanghai Health System Outstanding Academic Leader Training Program (XBR2013114 to Feng, J.); and the National Natural Science Foundation of China (U1602221 and 81325016 to Chen, C., and 81672624 to Feng, J.). In addition, Zhou, J. received support from the National Institutes of Health (P30 DA028821 and R01 DA038446) and a Cancer Prevention Research Institute of Texas (CPRIT) award. ; This work was supported by grants from "Personalized Medicines – Molecular Signature-based Drug Discovery and Development," a Strategic Priority Research Program of the Chinese Academy of Sciences (XDA12010303 to Chen, C.); The Shanghai Health System Outstanding Academic Leader Training Program (XBR2013114 to Feng, J.); and the National Natural Science Foundation of China (U1602221 and 81325016 to Chen, C., and 81672624 to Feng, J.). In addition, Zhou, J. received support from the National Institutes of Health (P30 DA028821 and R01 DA038446) and a Cancer Prevention Research Institute of Texas (CPRIT) award. |
| 源URL | [http://159.226.149.26:8080/handle/152453/11985]  |
| 专题 | 昆明动物研究所_动物模型与人类重大疾病机理重点实验室 昆明动物研究所_肿瘤生物学 |
| 作者单位 | 1.Fengxian District Center Hospital Graduate Student Training Base, Jinzhou Medical University, Shanghai, China, 201499 2.Chemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, Texas, 77555, United States 3.Department of Laboratory Medicine & Central Laboratory, Southern Medical University Affiliated Fengxian Hospital, Shanghai, China, 201499 4.Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences and Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming, China, 650223 5.Department of Laboratory Medicine, Huizhou No.3 People's Hospital, Affiliated hospital of Guangzhou Medical University, Huizhou, Guangdong, China, 516002 |
| 推荐引用方式 GB/T 7714 | Feng J*,Chen CS*,Ding Y,et al. YD277 Suppresses Triple-Negative Breast Cancer Partially Through Activating the Endoplasmic Reticulum Stress Pathway[J]. Theranostics,2017,7(8):2339-2349. |
| APA | Feng J*.,Chen CS*.,Ding Y.,Zhou WH.,Liu R.,...&Chen ZK.(2017).YD277 Suppresses Triple-Negative Breast Cancer Partially Through Activating the Endoplasmic Reticulum Stress Pathway.Theranostics,7(8),2339-2349. |
| MLA | Feng J*,et al."YD277 Suppresses Triple-Negative Breast Cancer Partially Through Activating the Endoplasmic Reticulum Stress Pathway".Theranostics 7.8(2017):2339-2349. |
入库方式： OAI收割
来源：昆明动物研究所
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