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Development of cell-active N6-methyladenosine RNA demethylase FTO inhibitor.

Journal of the American Chemical Society (2012-10-11)
Baoen Chen, Fei Ye, Lu Yu, Guifang Jia, Xiaotian Huang, Xueju Zhang, Shuying Peng, Kai Chen, Meining Wang, Shouze Gong, Ruihan Zhang, Jinya Yin, Haiyan Li, Yiming Yang, Hong Liu, Jiwen Zhang, Haiyan Zhang, Ao Zhang, Hualiang Jiang, Cheng Luo, Cai-Guang Yang
ABSTRACT

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.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Rhein
Sigma-Aldrich
Rhein, technical grade
Supelco
Rhein, analytical standard

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