Isochromanoindolenines suppress triple-negative breast cancer cell proliferation partially via inhibiting Akt activation

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	Isochromanoindolenines suppress triple-negative breast cancer cell proliferation partially via inhibiting Akt activation
	Jiang, XY; Zhi, X; Zhang, PX; Zhou, ZM; Ye, JX; Gao, Y; Wang, XY; Yang, CY; Chen, HJ; Liu, R; Chen, CS
	2021
发表期刊	INTERNATIONAL JOURNAL OF BIOLOGICAL SCIENCES
ISSN	1449-2288
卷号	17 期号:4 页码:986-994
摘要	As the most malignant subtype of breast cancers, triple-negative breast cancer (TNBC) lacks effective targeted therapeutics clinically to date. In this study, one lead compound FZU-0025-065 with isochromanoindolenine scaffold was identified by a cell-based screening. Among nine breast cancer cell lines tested, TNBC are the most sensitive cell lines to FZU-0025-065. FZU-0025-065 inhibits TNBC cell growth in a time- and dosage-dependent manner. FZU-0025-065 suppresses the expression of cell cycle dependent kinase 4 (CDK4), Cyclin D1 and Cyclin B1; meanwhile, elevates the expression of cell cycle dependent kinase inhibitor p21 and p27. Importantly, we found that FZU-0025-065 suppresses AKT activation in a time- and dosage-dependent manner. Over-expression of constitutive active AKT partially rescues FZU-0025-065 induced cell growth inhibition in MDA-MB-468 cells, indicating FZU-0025-065 suppresses TNBC cell growth partially via inhibiting AKT activation. Finally, FZU-0025-065 suppresses TNBC cell growth in a xenograft mouse model. Taken together, our findings suggested that isochromanoindolenine derivative FZU-0025-065 inhibits TNBC via suppressing the AKT signaling and that FZU-0025-065 may be useful for TNBC treatment.
收录类别	sci
语种	英语
文献类型	期刊论文
条目标识符	http://ir.kiz.ac.cn/handle/152453/13675
专题	科研部门_肿瘤生物学（陈策实）
推荐引用方式 GB/T 7714	Jiang, XY,Zhi, X,Zhang, PX,et al. Isochromanoindolenines suppress triple-negative breast cancer cell proliferation partially via inhibiting Akt activation[J]. INTERNATIONAL JOURNAL OF BIOLOGICAL SCIENCES,2021,17(4):986-994.
APA	Jiang, XY.,Zhi, X.,Zhang, PX.,Zhou, ZM.,Ye, JX.,...&Chen, CS.(2021).Isochromanoindolenines suppress triple-negative breast cancer cell proliferation partially via inhibiting Akt activation.INTERNATIONAL JOURNAL OF BIOLOGICAL SCIENCES,17(4),986-994.
MLA	Jiang, XY,et al."Isochromanoindolenines suppress triple-negative breast cancer cell proliferation partially via inhibiting Akt activation".INTERNATIONAL JOURNAL OF BIOLOGICAL SCIENCES 17.4(2021):986-994.

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