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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
LI WANSHUAI; SONG RAN; FANG XIANYING; WANG LU; CHEN WEI; Tang PP(汤平平); Yu B(俞飚); SUN YANG; XU QIANG
2012
发表期刊Biochem. Pharmacol.
ISSN0006-2952
卷号84期号:2页码:172-181
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.
学科领域生命有机化学
部门归属南京大学; 中科院上海有机化学研究所
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收录类别SCI
语种英语
WOS记录号WOS:000304843100004
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被引频次:8[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.sioc.ac.cn/handle/331003/28491
专题生命有机化学国家重点实验室
通讯作者Yu B(俞飚); SUN YANG; XU QIANG
推荐引用方式
GB/T 7714
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.
APA LI WANSHUAI.,SONG RAN.,FANG XIANYING.,WANG LU.,CHEN WEI.,...&XU QIANG.(2012).SBF-1, a synthetic steroidal glycoside, inhibits melanoma growth and metastasis through blocking interaction between PDK1 and AKT3.Biochem. Pharmacol.,84(2),172-181.
MLA LI WANSHUAI,et al."SBF-1, a synthetic steroidal glycoside, inhibits melanoma growth and metastasis through blocking interaction between PDK1 and AKT3".Biochem. Pharmacol. 84.2(2012):172-181.
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