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PDBsum entry 4zs3

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Fluorescent protein/inhibitor PDB id
4zs3
Contents
Protein chain
432 a.a.
Ligands
AKG
A4F
Metals
_MN
Waters ×52

References listed in PDB file
Key reference
Title Fluorescein derivatives as bifunctional molecules for the simultaneous inhibiting and labeling of fto protein.
Authors T.Wang, T.Hong, Y.Huang, H.Su, F.Wu, Y.Chen, L.Wei, W.Huang, X.Hua, Y.Xia, J.Xu, J.Gan, B.Yuan, Y.Feng, X.Zhang, C.G.Yang, X.Zhou.
Ref. J Am Chem Soc, 2015, 137, 13736-13739. [DOI no: 10.1021/jacs.5b06690]
PubMed id 26457839
Abstract
The FTO protein is unequivocally reported to play a critical role in human obesity and in the regulation of cellular levels of m(6)A modification, which makes FTO a significant and worthy subject of study. Here, we identified that fluorescein derivatives can selectively inhibit FTO demethylation, and the mechanisms behind these activities were elucidated after we determined the X-ray crystal structures of FTO/fluorescein and FTO/5-aminofluorescein. Furthermore, these inhibitors can also be applied to the direct labeling and enrichment of FTO protein combined with photoaffinity labeling assay.
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