Gambogic acid inhibits Hsp90 and deregulates TNF-alpha/NF-kappa B in HeLa cells

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	Gambogic acid inhibits Hsp90 and deregulates TNF-alpha/NF-kappa B in HeLa cells
	Zhang, L. R. ; Yi, Y. T. ; Chen, J. J. ; Sun, Y. F. ; Guo, Q. J. ; Zheng, Z. H. ; Song, S. Y. ; Zheng ZH(郑忠辉)
刊名	http://dx.doi.org/10.1016/j.bbrc.2010.11.018
	2010-12-17
关键词	MOLECULAR CHAPERONE ATPASE ACTIVITY CANCER CELLS BINDING APOPTOSIS RADICICOL PROTEINS ARREST GROWTH
英文摘要	National Natural Science Foundation of China [30973566, 30873148, 90913024]; Natural Science Foundation of Fujian Province of China [2010J01227]; Science and Technology Foundation of Xiamen [3502Z20093014]; Gambogic acid (GB) is an important anti-cancer drug candidate, but the target protein by which it exerts its anti-cancer effects has not been identified. This study is the first to show that GB inhibits heat shock protein 90 (Hsp90) and down-regulates TNF-alpha/NF-kappa B in He La cells. The effects of GB on Hsp90 were studied by characterizing its physical interactions with Hsp90 upon binding, the noncompetitive inhibition of Hsp90 ATPase activity, and the degradation of Hsp90 client proteins (i.e., Akt, IKK) in HeLa cells. GB seems to bind to the N-terminal ATP-binding domain of Hsp90. Additionally, GB suppresses the activation of TNF-alpha/NF-kappa B and decreases XIAP expression levels and the ratio of Bcl-2/Bax, which in turn induces HeLa cell apoptosis. Thus, GB represents a promising therapeutic agent for cancer; it may also be useful as a probe to increase understanding of the biological functions of Hsp90. (C) 2010 Elsevier Inc. All rights reserved.
语种	英语
内容类型	期刊论文
源URL	[http://dspace.xmu.edu.cn/handle/2288/65488]
专题	生命科学－已发表论文
推荐引用方式 GB/T 7714	Zhang, L. R.,Yi, Y. T.,Chen, J. J.,et al. Gambogic acid inhibits Hsp90 and deregulates TNF-alpha/NF-kappa B in HeLa cells[J]. http://dx.doi.org/10.1016/j.bbrc.2010.11.018,2010.
APA	Zhang, L. R..,Yi, Y. T..,Chen, J. J..,Sun, Y. F..,Guo, Q. J..,...&郑忠辉.(2010).Gambogic acid inhibits Hsp90 and deregulates TNF-alpha/NF-kappa B in HeLa cells.http://dx.doi.org/10.1016/j.bbrc.2010.11.018.
MLA	Zhang, L. R.,et al."Gambogic acid inhibits Hsp90 and deregulates TNF-alpha/NF-kappa B in HeLa cells".http://dx.doi.org/10.1016/j.bbrc.2010.11.018 (2010).