Combination therapy of RY10-4 with the gamma-secretase inhibitor DAPT shows promise in treating HER2-amplified breast cancer

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作者信息关键词期刊信息基础信息归属信息摘要

成果类型：

期刊论文

作者：

Su, Feng;Zhu, Shilin;Ruan, Jinlan;Muftuoglu, Yagmur;Zhang, Longbo*;...

通讯作者：

Yuan, Qianying;Zhang, Longbo

作者机构：

[Su, Feng] Cent S Univ, Xiangya Hosp, Dept Emergency, Changsha, Hunan, Peoples R China.

[Zhu, Shilin] Hunan Univ Chinese Med, Affiliated Hosp 2, Changsha, Hunan, Peoples R China.

[Yuan, Qianying; Ruan, Jinlan] Huazhong Univ Sci & Technol, Dept Pharmacol, Wuhan 430074, Peoples R China.

[Muftuoglu, Yagmur; Yuan, Qianying] Yale Univ, Sch Med, Dept Pharmacol, New Haven, CT 06510 USA.

[Zhang, Longbo] Cent S Univ, Xiangya Hosp, Dept Neurosurg, Changsha, Hunan, Peoples R China.

通讯机构：

[Yuan, Qianying] H

[Yuan, Qianying] Y

[Zhang, Longbo] C

Huazhong Univ Sci & Technol, Dept Pharmacol, Wuhan 430074, Peoples R China.

Yale Univ, Sch Med, Dept Pharmacol, New Haven, CT 06510 USA.

语种：

英文

关键词：

Notch;RY10-4;breast cancer;resistance

期刊：

Oncotarget

ISSN：

1949-2553

年：

2016

卷：

期：

页码：

4142-4154

DOI：

10.18632/oncotarget.6769

基金类别：

National Nature Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [81173093]

机构署名：

本校为其他机构

院系归属：

第二中医临床医学院

摘要：

RY10-4, a novel protoapigenone analog, shows potent cytotoxicity against human breast cancer cells. However, breast cancer cell lines overexpressing human epidermal growth factor receptor 2 (HER2), SKBR3 and BT474, showed less sensitivity to RY10-4 when compared to breast cancer cells lines expressing lower levels of HER2, such as MDA-MB-231 and MCF-7 cells. This was associated with aberrant hyperactivity in Notch signaling in cells treated with RY10-4, since treatment with RY10-4 causes an increase in Notch activity by 2-to3.5-fold in SKBR3 and BT474 cell lines. The increase in activity was a...

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Combination therapy of RY10-4 with the gamma-secretase inhibitor DAPT shows promise in treating HER2-amplified breast cancer

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