Identification of A Novel Small-Molecule Binding Site of the Fat Mass and Obesity Associated Protein (FTO)

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• 作者：Wu He ; Bin Zhou ; Weijia Liu ; Meizi Zhang ; Zhenhua Shen ; Zhifu Han ; Qingwei Jiang ; Qinghua Yang ; Chuanjun Song ; Ruiyong Wang ; Tianhui Niu ; Shengna Han ; Lirong Zhang ; Jie Wu ; Feima Guo ; Renbin Zhao ; Wenquan Yu ; Jijie Chai ; Junbiao Chang
• 刊名：Journal of Medicinal Chemistry
• 出版年：2015
• 出版时间：September 24, 2015
• 年：2015
• 卷：58
• 期：18
• 页码：7341-7348
• 全文大小：462K
• ISSN：1520-4804

文摘

N-(5-Chloro-2,4-dihydroxyphenyl)-1-phenylcyclobutanecarboxamide (N-CDPCB, 1a) is found to be an inhibitor of the fat mass and obesity associated protein (FTO). The crystal structure of human FTO with 1a reveals a novel binding site for the FTO inhibitor and defines the molecular basis for recognition by FTO of the inhibitor. The identification of the new binding site offers new opportunities for further development of selective and potent inhibitors of FTO, which is expected to provide information concerning novel therapeutic targets for treatment of obesity or obesity-associated diseases.