4ZS2

Structural complex of FTO/fluorescein

4ZS2 の概要

• エントリーDOI: 10.2210/pdb4zs2/pdb
• 関連するPDBエントリー: 4ZS3
• 分子名称: Alpha-ketoglutarate-dependent dioxygenase FTO, 2-OXOGLUTARIC ACID, 2-(6-HYDROXY-3-OXO-3H-XANTHEN-9-YL)-BENZOIC ACID, ... (5 entities in total)
• 機能のキーワード: inhibitor, fluorescein, fluorescent protein-inhibitor complex, fluorescent protein/inhibitor
• 由来する生物種: Homo sapiens (Human)
• 細胞内の位置: Nucleus : Q9C0B1
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 55467.31

構造登録者

Wang, T.,Hong, T.,Huang, Y.,Yang, C.G.,Zhou, X. (登録日: 2015-05-13, 公開日: 2015-11-04, 最終更新日: 2024-10-30)

主引用文献

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

実験手法

X-RAY DIFFRACTION (2.16 Å)