Spectroscopic probing of recognition of the G-quadruplex in c-kit promoter by small-molecule natural products

doi:10.1016/j.ijbiomac.2012.02.029

	Spectroscopic probing of recognition of the G-quadruplex in c-kit promoter by small-molecule natural products
	Cui, Xiaojie; Lin, Sen; Yuan, Gu
刊名	INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
	2012-05-01
卷号	50 期号:4 页码:996-1001
关键词	G-quadruplex C-kit Oncogene Esi-ms Cd Small Molecules Autodock3
ISSN号	0141-8130
DOI	10.1016/j.ijbiomac.2012.02.029
文献子类	Article
英文摘要	The c-kit oncogene plays important roles in cell growth and proliferation which is associated with many human tumors. In this study, electrospray ionization mass spectrometry (ESI-MS) and circular dichroism (CD) spectroscopy were used to evaluate the formation and recognition of the G-quadruplex by d(AGGGAGGGCGCTGGGAGGAGGG) in the promoter region of the c-kit oncogene. Among the twelve small natural molecules studied, three crescent-shaped small molecules (chelerythrine, jatrorrhizine and berberine, named as P1-P3) and one flexible cyclic small molecule (fangchinoline, named as P4) were found to bind to the G-quadruplex with high affinities. The melting experiments demonstrate that P1-P4 can significantly enhance the stability of the G-quadruplex with the ordering of P1 approximate to P4> P3> P2. Further insight into the binding mode of small molecules with the G-quadruplex by Autodock3 analysis reveals that P1-P3 prefer the end-stacking mode with the G-quadruplex through pi-pi interaction and P4 prefers to insert into the groove outside the G-tetrads. Thus, our research finds that four ligands (P1-P4) from small natural molecules have high affinity to, and can significantly enhance the stability of the G-quadruplex in the promoter region of the c-kit oncogene. (C) 2012 Elsevier B.V. All rights reserved.
WOS关键词	IONIZATION MASS-SPECTROMETRY ; GASTROINTESTINAL STROMAL TUMORS ; TYROSINE KINASE ; BINDING ; REGION ; GENE ; DNA ; STABILIZATION ; MUTATIONS ; COMPLEXES
WOS研究方向	Biochemistry & Molecular Biology
语种	英语
出版者	ELSEVIER SCIENCE BV
WOS记录号	WOS:000304230000017
内容类型	期刊论文
源URL	[http://cas-ir.dicp.ac.cn/handle/321008/167288]
专题	大连化学物理研究所_中国科学院大连化学物理研究所
通讯作者	Yuan, Gu
作者单位	Peking Univ, Beijing Natl Lab Mol Sci, Key Lab Bioorgan Chem & Mol Engn, Coll Chem & Mol Engn,Dept Chem Biol,Minist Educ, Beijing 100871, Peoples R China
推荐引用方式 GB/T 7714	Cui, Xiaojie,Lin, Sen,Yuan, Gu. Spectroscopic probing of recognition of the G-quadruplex in c-kit promoter by small-molecule natural products[J]. INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES,2012,50(4):996-1001.
APA	Cui, Xiaojie,Lin, Sen,&Yuan, Gu.(2012).Spectroscopic probing of recognition of the G-quadruplex in c-kit promoter by small-molecule natural products.INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES,50(4),996-1001.
MLA	Cui, Xiaojie,et al."Spectroscopic probing of recognition of the G-quadruplex in c-kit promoter by small-molecule natural products".INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES 50.4(2012):996-1001.