Development of Cell-Active N-6-Methyladenosine RNA Demethylase FTO   Inhibitor

doi:10.1021/ja3064149

CORC > 北京大学 > 化学与分子工程学院

	Development of Cell-Active N-6-Methyladenosine RNA Demethylase FTO Inhibitor
	Chen, Baoen ; Ye, Fei ; Yu, Lu ; Jia, Guifang ; Huang, Xiaotian ; Zhang, Xueju ; Peng, Shuying ; Chen, Kai ; Wang, Meining ; Gong, Shouze ; Zhang, Ruihan ; Yin, Jinya ; Li, Haiyan ; Yang, Yiming ; Liu, Hong ; Zhang, Jiwen ; Zhang, Haiyan ; Zhang, Ao ; Jiang, Hualiang ; Luo, Cheng ; Yang, Cai-Guang
刊名	journal of the american chemical society
	2012
关键词	NUCLEIC-ACID DEMETHYLASE OBESITY-ASSOCIATED FTO REPAIR ENZYME ALKB OXIDATIVE DEMETHYLATION CRYSTAL-STRUCTURES MASS-SPECTROMETRY ESCHERICHIA-COLI COMMON VARIANT ADULT OBESITY FAT MASS
DOI	10.1021/ja3064149
英文摘要	The direct nucleic acid repair dioxygenase FTO is an enzyme that demethylates N-6-methyladenosine (m(6)A) residues in mRNA in vitro and inside cells. FTO is the first RNA demethylase discovered that also serves a major regulatory function in mammals. Together with structure-based virtual screening and biochemical analyses, we report the first identification of several small-molecule inhibitors of human FTO demethylase. The most potent compound, the natural product rhein, which is neither a structural mimic of 2-oxoglutarate nor a chelator of metal ion, competitively binds to the FTO active site in vitro. Rhein also exhibits good inhibitory activity on m(6)A demethylation inside cells. These studies shed light on the development of powerful probes and new therapies for use in RNA biology and drug discovery.; Chemistry, Multidisciplinary; SCI(E); EI; 21; ARTICLE; 43; 17963-17971; 134
语种	英语
内容类型	期刊论文
源URL	[http://ir.pku.edu.cn/handle/20.500.11897/229584]
专题	化学与分子工程学院
推荐引用方式 GB/T 7714	Chen, Baoen,Ye, Fei,Yu, Lu,et al. Development of Cell-Active N-6-Methyladenosine RNA Demethylase FTO Inhibitor[J]. journal of the american chemical society,2012.
APA	Chen, Baoen.,Ye, Fei.,Yu, Lu.,Jia, Guifang.,Huang, Xiaotian.,...&Yang, Cai-Guang.(2012).Development of Cell-Active N-6-Methyladenosine RNA Demethylase FTO Inhibitor.journal of the american chemical society.
MLA	Chen, Baoen,et al."Development of Cell-Active N-6-Methyladenosine RNA Demethylase FTO Inhibitor".journal of the american chemical society (2012).