Fluorescein Derivatives as Bifunctional Molecules for the Simultaneous Inhibiting and Labeling of FTO Protein

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• 作者：Tianlu Wang ; Tingting Hong ; Yue Huang ; Haomiao Su ; Fan Wu ; Yi Chen ; Lai Wei ; Wei Huang ; Xiaoluan Hua ; Yu Xia ; Jinglei Xu ; Jianhua Gan ; Bifeng Yuan ; Yuqi Feng ; Xiaolian Zhang ; Cai-Guang Yang ; Xiang Zhou
• 刊名：Journal of the American Chemical Society
• 出版年：2015
• 出版时间：November 4, 2015
• 年：2015
• 卷：137
• 期：43
• 页码：13736-13739
• 全文大小：324K
• ISSN：1520-5126

文摘

The FTO protein is unequivocally reported to play a critical role in human obesity and in the regulation of cellular levels of m⁶A 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.