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学科主题: 生命有机化学
题名: SBF-1, a synthetic steroidal glycoside, inhibits melanoma growth and metastasis through blocking interaction between PDK1 and AKT3
其他题名: SBF-1, 一种合成的甾体皂苷, 能通过阻断PDK1和AKT3之间的相互作用抑制黑色素瘤的生长和转移
作者: LI WANSHUAI ; SONG RAN ; FANG XIANYING ; WANG LU ; CHEN WEI ; Tang PP(汤平平) ; Yu B(俞飚) ; SUN YANG ; XU QIANG
通讯作者: 俞飚 ; SUN YANG ; XU QIANG
刊名: Biochem. Pharmacol.
发表日期: 2012
卷: 84, 期:2, 页:172-181
收录类别: SCI
部门归属: 南京大学; 中科院上海有机化学研究所
英文摘要: In the present study, we demonstrate that SBF-1, a synthetic steroidal glycoside, has a strong antitumor activity against melanoma cells in vitro and in vivo. SBF-1 induced cell cycle arrest with a reduced expression of various cell cycle related proteins in B16BL6 melanoma cells without causing apoptosis. SBF-1 dramatically inhibited kinase activity of 3-phosphoinositide dependent protein kinase 1 (PDK1) and thus down-regulated phosphorylation of protein kinase B (AKT). Among three known isoforms of PDK1 only interacted with AKT3 in B16BL6 melanoma cells, and SBF-1 almost completely blocked this interaction. In addition, adhesion to fibronectin and expression of integrin alpha 4 were significantly reduced in a concentration-dependent manner. Knockdown of AKT3 resulted in the decrease in integrin a4 expression and cell adhesion. Moreover, SBF-1 inhibited the growth of melanoma xenografts and down-regulated the phosphorylation of Ala in vivo. In a mouse model of spontaneous metastasis, SBF-1 at very low doses of 1 and 3 mu g/kg enormously inhibited melanoma metastasis into draining popliteal lymph nodes. Taken together, this study shows a small molecular compound SBF-1 with a very strong anti-melanoma activity both in vitro and in vivo. its mechanism underlying such antitumor effect is related to the blockage of the interaction between PDK1 and AKT3. (C) 2012 Elsevier Inc. All rights reserved.
语种: 英语
相关网址: 查看原文
WOS记录号: WOS:000304843100004
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/28491
Appears in Collections:生命有机化学国家重点实验室_期刊论文

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Recommended Citation:
LI WANSHUAI,SONG RAN,FANG XIANYING,et al. SBF-1, a synthetic steroidal glycoside, inhibits melanoma growth and metastasis through blocking interaction between PDK1 and AKT3[J]. Biochem. Pharmacol.,2012,84(2):172-181.
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