4ZS3

Structural complex of 5-aminofluorescein bound to the FTO protein

Summary for 4ZS3

• Entry DOI: 10.2210/pdb4zs3/pdb
• Related: 4ZS2
• Descriptor: Alpha-ketoglutarate-dependent dioxygenase FTO, 2-OXOGLUTARIC ACID, 5-amino-2-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoic acid, ... (5 entities in total)
• Functional Keywords: fluorescent protein-inhibitor complex, fluorescent protein/inhibitor
• Biological source: Homo sapiens (Human)
• Cellular location: Nucleus : Q9C0B1
• Total number of polymer chains: 1
• Total formula weight: 55482.32

Authors

Wang, T.,Hong, T.,Huang, Y.,Yang, C.G.,Zhou, X. (deposition date: 2015-05-13, release date: 2015-11-04, Last modification date: 2024-11-06)

Primary citation

Wang, T.,Hong, T.,Huang, Y.,Su, H.,Wu, F.,Chen, Y.,Wei, L.,Huang, W.,Hua, X.,Xia, Y.,Xu, J.,Gan, J.,Yuan, B.,Feng, Y.,Zhang, X.,Yang, C.G.,Zhou, X.
Fluorescein Derivatives as Bifunctional Molecules for the Simultaneous Inhibiting and Labeling of FTO Protein
J.Am.Chem.Soc., 137:13736-13739, 2015

PubMed 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.

PubMed: 26457839
DOI: 10.1021/jacs.5b06690

Experimental method

X-RAY DIFFRACTION (2.45 Å)