Details

Autor(en) / Beteiligte

• Qiao, Yan
• Zhou, Bin
• Zhang, Meizi
• Liu, Weijia
• Han, Zhifu
• Song, Chuanjun
• Yu, Wenquan
• Yang, Qinghua
• Wang, Ruiyong
• Wang, Shaomin
• Shi, Shuai
• Zhao, Renbin
• Chai, Jijie
• Chang, Junbiao

Titel

A Novel Inhibitor of the Obesity-Related Protein FTO

Ist Teil von

• Biochemistry (Easton), 2016-03, Vol.55 (10), p.1516-1522

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2016

Quelle

MEDLINE

Beschreibungen/Notizen

• FeII and α-ketoglutarate-dependent fat mass and obesity associated protein (FTO)-dependent demethylation of m6A is important for regulation of mRNA splicing and adipogenesis. Developing FTO-specific inhibitors can help probe the biology of FTO and unravel novel therapeutic targets for treatment of obesity or obesity-associated diseases. In the present paper, we have identified that 4-chloro-6-(6′-chloro-7′-hydroxy-2′,4′,4′-trimethyl-chroman-2′-yl)­benzene-1,3-diol (CHTB) is an inhibitor of FTO. The crystal structure of CHTB complexed with human FTO reveals that the novel small molecule binds to FTO in a specific manner. The identification of the novel small molecule offers opportunities for further development of more selective and potent FTO inhibitors.