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

CORC > 北京大学 > 化学与分子工程学院

	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	国际生物大分子杂志
	2012
关键词	G-quadruplex C-kit oncogene ESI-MS CD Small molecules Autodock3 IONIZATION MASS-SPECTROMETRY GASTROINTESTINAL STROMAL TUMORS TYROSINE KINASE BINDING REGION GENE DNA STABILIZATION MUTATIONS COMPLEXES
DOI	10.1016/j.ijbiomac.2012.02.029
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.; http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000304230000017&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=8e1609b174ce4e31116a60747a720701 ; Biochemistry & Molecular Biology; SCI(E); PubMed; 9; ARTICLE; 4; 996-1001; 50
语种	英语
内容类型	期刊论文
源URL	[http://ir.pku.edu.cn/handle/20.500.11897/149907]
专题	化学与分子工程学院
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]. 国际生物大分子杂志,2012.
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.国际生物大分子杂志.
MLA	Cui, Xiaojie,et al."Spectroscopic probing of recognition of the G-quadruplex in c-kit promoter by small-molecule natural products".国际生物大分子杂志 (2012).