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	Inhibitation and Binding of Rugulosin with N-Hsp90
	Chen, Jun-Jie ; Yi, Yu-Ting ; Yu, Miao ; Xue, Shao-Long ; Xiong, Qian-Qian ; He, Xiao-Meng ; Zhang, Lian-Ru ; Zhang LR(张连茹)
	2010-12-11
关键词	Rugulosin Hsp90 Fluorescence spectroscopy Circular dichroism spectroscopy Surface plasmon resonance
英文摘要	Rugulosin firstly isolated from the metabolites of Penicillium rugulosum Thom has a strong inhibitory activity on Streptococcus and Corynebacterium. Heat shock protein 90(Hsp90) is a molecular chaperone required for the stability and function of a number of signalling proteins and protein kinases that promote cancer cell growth or survival. By molecular docking, we found the combination between Rugulosin and N-Hsp90 (N-terminal of Hsp90, the ATPase activity domain). Rugulosin showed strong inhibition to ATPase activity of Hsp90 and the IC(50) was 22. 3 mu mol/L in vitro experiments. In this study, the interaction mechanism of Rugulosin with N-Hsp90 was investigated by fluorescence, ForteBio Octet, circular dichroism, UV-Visible absorption spectroscopy, SPR technology and Western Blot. Fluorescence spectra experiment results showed that Rugulosin caused a strong fluorescence quenching on intrinsic fluorescence of Hsp90 by static quenching method. Thermodynamic analysis signified the binding mechanism was hydrogen forces and dissociation constant was 22. 4 mu mol/L, which was 85. 9 mu mol/L calculated from ForteBio Octet method. Circular dichroism spectra detected the a-helix of N-Hsp90 reduced as the concentration of Rugulosin increased. Rugulosin could also down-regulate the expression of the client protein Akt and Raf-1 in HeLa cells. This study illustrates that Ruglulosin, which inhibited the ATPase activity of Hsp90 through interacting with N-Hsp90, may be a potential inhibitor of Hsp90.
语种	英语
出版者	HIGHER EDUCATION PRESS
内容类型	期刊论文
源URL	[http://dspace.xmu.edu.cn/handle/2288/11877]
专题	生命科学－已发表论文
推荐引用方式 GB/T 7714	Chen, Jun-Jie,Yi, Yu-Ting,Yu, Miao,et al. Inhibitation and Binding of Rugulosin with N-Hsp90[J],2010.
APA	Chen, Jun-Jie.,Yi, Yu-Ting.,Yu, Miao.,Xue, Shao-Long.,Xiong, Qian-Qian.,...&张连茹.(2010).Inhibitation and Binding of Rugulosin with N-Hsp90..
MLA	Chen, Jun-Jie,et al."Inhibitation and Binding of Rugulosin with N-Hsp90".(2010).

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