Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 58, Issue 18, Pages 7341-7348Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b00702
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Funding
- National Natural Science Foundation of China [81330075]
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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 la 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.
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