Fluorescein Derivatives as Bifunctional Molecules for the Simultaneous Inhibiting and Labeling of FTO Protein
                                
                                    
                                        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                                    
                                    
                                        DOI:10.1021/jacs.5b06690
                                    
                                    
                                        日期:2015.11.4
                                    
                                    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.