Journal of medicinal chemistry, 2015-09, Vol.58 (18), p.7341-7348
2015
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Details
- Autor(en) / Beteiligte
- Titel
- Identification of A Novel Small-Molecule Binding Site of the Fat Mass and Obesity Associated Protein (FTO)
- Ist Teil von
- Journal of medicinal chemistry, 2015-09, Vol.58 (18), p.7341-7348
- Ort / Verlag
- United States: American Chemical Society
- Erscheinungsjahr
- 2015
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- 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.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0022-2623eISSN: 1520-4804DOI: 10.1021/acs.jmedchem.5b00702Titel-ID: cdi_proquest_miscellaneous_1716937854
- Format
- –
- Schlagworte
- 3T3-L1 Cells, Alpha-Ketoglutarate-Dependent Dioxygenase FTO, Aminophenols - chemical synthesis, Aminophenols - chemistry, Aminophenols - pharmacology, Anilides - chemical synthesis, Anilides - chemistry, Anilides - pharmacology, Animals, Binding Sites, Crystallography, X-Ray, Databases, Chemical, Humans, Methylation, Mice, Models, Molecular, Protein Binding, Proteins - antagonists & inhibitors, Proteins - chemistry, RNA - chemistry, RNA, Messenger - metabolism