Deguelin suppresses non-small cell lung cancer by inhibiting EGFR signaling and promoting GSK3β/FBW7-mediated Mcl-1 destabilization

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成果类型：

期刊论文

作者：

Gao, Feng;Yu, Xinfang;Li, Ming;Zhou, Li;Liu, Wenbin;...

通讯作者：

Liu, HD;Li, W

作者机构：

[Liu, Haidan; Gao, Feng] Cent South Univ, Dept Cardiovasc Surg, Xiangya Hosp 2, Changsha 410011, Hunan, Peoples R China.

[Liu, Haidan; Gao, Feng] Cent South Univ, Clin Ctr Gene Diag & Therapy, Xiangya Hosp 2, Changsha 410011, Hunan, Peoples R China.

[Gao, Feng] Cent South Univ, Dept Ultrasonog, Xiangya Hosp 3, Changsha 410013, Hunan, Peoples R China.

[Yu, Xinfang] Cleveland Clin, Lerner Res Inst, Dept Canc Biol, 9500 Euclid Ave, Cleveland, OH 44195 USA.

[Li, Ming] Changsha Stomatol Hosp, Changsha 410004, Hunan, Peoples R China.

通讯机构：

[Liu, HD ; Li, W ] C

Cent South Univ, Dept Cardiovasc Surg, Xiangya Hosp 2, Changsha 410011, Hunan, Peoples R China.

Cent South Univ, Clin Ctr Gene Diag & Therapy, Xiangya Hosp 2, Changsha 410011, Hunan, Peoples R China.

Cent South Univ, Dept Radiol, Xiangya Hosp 3, Changsha 410013, Hunan, Peoples R China.

语种：

英文

期刊：

CELL DEATH & DISEASE

ISSN：

2041-4889

年：

2020

卷：

期：

页码：

143

DOI：

10.1038/s41419-020-2344-0

基金类别：

This work was supported by the National Natural Science Foundation of China (Nos. 81572280, 81904262, and 81972837), the Natural Science Foundation of Hunan Province (2018JJ3787, 2018JJ2604, 2019JJ40420, 2019JJ50682), and the Natural Science Foundation of Changsha Science and Technology Bureau (kq1701018).

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摘要：

AbstractActivating mutations of epidermal growth factor receptor (EGFR) play crucial roles in the oncogenesis of human non-small cell lung cancer (NSCLC). By screening 79 commercially available natural products, we found that the natural compound deguelin exhibited a profound anti-tumor effect on NSCLC via directly down-regulating of EGFR-signaling pathway. Deguelin potently inhibited in vitro EGFR kinase activity of wild type (WT), exon 19 deletion, and L858R/T790M-mutated EGFR. The in silico docking study indicated that deguelin was docked in...

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Deguelin suppresses non-small cell lung cancer by inhibiting EGFR signaling and promoting GSK3β/FBW7-mediated Mcl-1 destabilization

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