Inhibitation and Binding of Rugulosin  with N-Hsp90

Chem. J. Chinese Universities ›› 2011, Vol. 32 ›› Issue (1): 88.

• Articles • Previous Articles Next Articles

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*

School of Life Sciences, Xiamen University, Xiamen 361005, China

Received:2010-03-30 Revised:2010-09-13 Online:2011-01-10 Published:2010-12-11
Contact: ZHANG Lian-Ru E-mail:ru898@126.com
Supported by:
国家自然科学基金(批准号: 30873148, 30973566, 30921005, 90913024)和国家“重大新药创制”科技重大专项(批准号: 2009ZX09103-083)资助.

Abstract

Abstract: By Docking simulation, We find the combination between Rugulosin and N-terminal of Hsp90 which is the ATPase activity domain. Rugulosin show a strong inhibition to ATPase activity of Hsp90 and the IC50 is 22.27μM in vitro experiment. In this study, we do a research on the interaction mechanism of Rugulosin with NHsp90 protein (N-Terminal of Hsp90)by fluorescence, circular dichroism, UV - visible absorption spectroscopy, and SPR technology. fluorescence spectra experiment results show that Rugulosin cause a strong fluorescence quenching on endogenous fluorescence of Hsp90 by static quenching method. Thermodynamic analysis signify the Binding mechanism is electrostatic forces and dissociation constant is 22.4 ± 0.17μM. Circular dichroism spectra detected the α-helix of NHsp90 reducing as the Rugulosin concentration increased, This study show that Rugulosin can make a combination with NHsp90, thereby inhibiting its ATPase activity. Ruglulosin may be a potential inhibitor of Hsp90.

Key words: Rugulosin, Hsp90, fluorescence spectroscopy, circular dichroism spectroscopy, UV-visible absorption spectra

TrendMD:

CHEN Jun-Jie, YI Yu-Ting, YU Miao, XUE Shao-Long, XIONG Qian-Qian, HE Xiao-Meng, ZHANG Lian-Ru*. Inhibitation and Binding of Rugulosin with N-Hsp90[J]. Chem. J. Chinese Universities, 2011, 32(1): 88.

[1]	TIAN Xia,YANG Fuqun,YUAN Wei,ZHAO Lei,YAO Lei,ZHEN Xiaoli,HAN Jianrong,LIU Shouxin. Synthesis, Structure and Recognition Properties of Macrocyclic Crown Ethers with Oxadiazole ^† [J]. Chem. J. Chinese Universities, 2020, 41(3): 490.
[2]	WANG Mengyu, CAO Simin, LI Haoyang, ZHANG Mengjie, LI Dong, ZHAO Zenan, XU Jianhua. Fluorescence Resonance Energy Transfer Between Coenzyme NADH and Tryptophan [J]. Chem. J. Chinese Universities, 2020, 41(11): 2473.
[3]	WEI Xin, DENG Yaoliang, ZHENG Xuming, ZHAO Yanying. Ground Structure and Excited State Proton Transfer Reaction of 2-Aminobenzothiazole [J]. Chem. J. Chinese Universities, 2019, 40(8): 1679.
[4]	SHI Penghui,BIAN Liujiao. Mechanism Study on the Interaction Between Cefoxitin and Metal β-Lactamase BcⅡ Based on Spectroscopic Methods and Computional Simulations^† [J]. Chem. J. Chinese Universities, 2018, 39(5): 971.
[5]	WANG Yan, CHEN Ping, WANG Yunfei, LIU Guiying, YANG Xi, SU Ying, LI Junyang, LIU Weiwei, LIN Lie. Spectral Characterization of the Interaction Between Methamphetamine and Serum Albumin^† [J]. Chem. J. Chinese Universities, 2018, 39(11): 2507.
[6]	CHEN Jingxin, LIAN Wenhua, CHENG Yuanchu, XU Jianhua, ZHANG Lianru. Effect of Curcumin on Yeast Cells by Fluorescence Analysis^† [J]. Chem. J. Chinese Universities, 2018, 39(1): 71.
[7]	ZHAO Bing, ZHUANG Xiaoyu, LIU Shu, ZHENG Zhong, LIU Zhiqiang, SONG Fengrui. Interaction Between 5-Furd and Cu,Zn-SOD1 by Ion Mobility Mass Spectrometry and Fluorescence Spectroscopy [J]. Chem. J. Chinese Universities, 2017, 38(8): 1341.
[8]	SUN Yan-Mei, WU Hai-Long, WANG Jian-Yao, YU Ru-Qin. Determination of Melatonin in Functional Food by Three-dimensional Fluorescence Spectroscopy Combined with Second-order Calibration Method [J]. Chem. J. Chinese Universities, 2013, 34(5): 1084.
[9]	HUANG Ying, WANG Juan, GUO Gai-Ying, TAO Zhu, XUE Sai-Feng, ZHU Qian-Jiang, ZHOU Qing-Di. Interaction of 6-Thioguanine with Cucurbit[7]uril and Bovine Serum Albumin by Spectroscopic Method [J]. Chem. J. Chinese Universities, 2013, 34(2): 375.
[10]	LI Hong-Liang, ZHANG Lin-Ya, ZHU Li-Yun, NI Cui-Xia, SHANG Han-Wu*. Interaction of Chemosensory Proteins of Apis cerana cerana with Special Ligands by Fluorescence Spectroscopy [J]. Chem. J. Chinese Universities, 2011, 32(6): 1284.
[11]	MA Ping, CHI Yan-Hua*, ZHUANG Jia, WANG Han, CHEN Liang, LIU Xu, DONG Fa-Qin. Spectroscopic Studies on the Interaction of Murexide and Murexide-Copper Complex with Human Serum Albumin [J]. Chem. J. Chinese Universities, 2009, 30(8): 1509.
[12]	GUO Wei, WU Yong-Quan, ZHENG Lü-Yin, XU Li-Rong, FAN Xiao-Lin*. Interaction of Keyhole Limpet Hemocyanin with Niclosamide and Its Derivative [J]. Chem. J. Chinese Universities, 2009, 30(7): 1314.
[13]	LIU Gen-Lan¹, NI Yong-Nian^1,2*. Fluorescence Spectrometric Study on the Interaction Between Umbelliferone and Bovine Serum Albumin with the Use of MCR-ALS [J]. Chem. J. Chinese Universities, 2008, 29(7): 1339.
[14]	ZHANG Li-Wei, ZHANG Xin-Xiang*. Interactions Between Fluoroquinolones and Bovine Serum Albumin by Fluorescence Method and Affinity Capillary Electrophoresis [J]. Chem. J. Chinese Universities, 2008, 29(4): 694.
[15]	ZHOU Jie, MENG Qing-Fan, TIAN Xiao-Le, CHENG Ying-Kun, JIANG Fu-Jia, LI Qing-Shan, TENG Li-Rong. Spectroscopic Characterization of An Antimicrobial Peptide(RTCⅠ) from Skin of Rana temporaria chensinensis, David* [J]. Chem. J. Chinese Universities, 2007, 28(6): 1064.

Inhibitation and Binding of Rugulosin with N-Hsp90

PDF (PC)

Knowledge

Abstract

Cite this article

share this article

References

Related Articles 15

Recommended Articles

Metrics

Comments