机构:[1]Lester and Sue Smith Breast Center, and Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, TX, 77030, USA.[2]Department of Oncology and Hematology, Hospital (TCM) Affiliated to Southwest Medical University, Luzhou, Sichuan, 646000, P. R. China.[3]Department of Systems Medicine and Bioengineering, Houston Methodist Research Institute, Houston, TX, 77030, USA.[4]Department of Dermatology, National Taiwan University Hospital and National Taiwan University College of Medicine, Taipei, 10002, Taiwan.
Ras GTPases are powerful drivers for tumorigenesis, but directly targeting Ras for treating cancer remains challenging. The growth and transforming activity of the aggressive basal-like breast cancer (BLBC) are driven by N-Ras. To target N-Ras in BLBC, this study screened existing pharmacologically active compounds for the new ability to induce N-Ras degradation, which led to the identification of flunarizine (FLN), previously approved for treating migraine and epilepsy. The FLN-induced N-Ras degradation was not affected by a 26S-proteasome inhibitor. Rather, it was blocked by autophagy inhibitors. Furthermore, N-Ras can be seen co-localized with active autophagosomes upon FLN treatment, suggesting that FLN alters the autophagy pathway to degrade N-Ras. Importantly, FLN treatment recapitulated the effect of N-RAS silencing in vitro by selectively inhibiting the growth of BLBC cells, but not that of breast cancer cells of other subtypes. In addition, in vivo FLN inhibited tumor growth of a BLBC xenograft model. In conclusion, this proof-of-principle study presents evidence that the autophagy pathway can be coerced by small molecule inhibitors, such as FLN, to degrade Ras as a strategy to treat cancer. FLN has low toxicity and should be further investigated to enrich the toolbox of cancer therapeutics.
基金:
This project was assisted by a P30 Cancer Center Support Grant from NCI (P30CA125123).
ECC was supported by The Susan G. Komen Foundation (SAC150059), DOD (W81XWH-16-1-0538), Nancy
Owen Memorial Foundation, NIH (R21CA185516, R21CA226567, and P50CA186784), and Cancer Prevention
and Research Institute of Texas (CPRIT, RP180844). We are particularly grateful for the support from the William
and Ella Owens Foundation. YHL was supported by Ministry of Science and Technology (MOST) of the Republic
of China under Grant No. MOST 103-2314-B-002-067-MY3 (Y-H. Liao).
语种:
外文
PubmedID:
中科院(CAS)分区:
出版当年[2018]版:
大类|3 区综合性期刊
小类|3 区综合性期刊
最新[2023]版:
大类|2 区综合性期刊
小类|2 区综合性期刊
第一作者:
第一作者机构:[1]Lester and Sue Smith Breast Center, and Department of Molecular and Cellular Biology, Baylor College of Medicine, Houston, TX, 77030, USA.
通讯作者:
推荐引用方式(GB/T 7714):
Ze-Yi Zheng,Jing Li,Fuhai Li,et al.Induction of N-Ras degradation by flunarizine-mediated autophagy.[J].Scientific reports.2018,8(1):16932.doi:10.1038/s41598-018-35237-2.
APA:
Ze-Yi Zheng,Jing Li,Fuhai Li,Yanqiao Zhu,Kemi Cui...&Yi-Hua Liao.(2018).Induction of N-Ras degradation by flunarizine-mediated autophagy..Scientific reports,8,(1)
MLA:
Ze-Yi Zheng,et al."Induction of N-Ras degradation by flunarizine-mediated autophagy.".Scientific reports 8..1(2018):16932