2. Academic Validation
  3. Fluorescein Derivatives as Bifunctional Molecules for the Simultaneous Inhibiting and Labeling of FTO Protein

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

  • J Am Chem Soc. 2015 Nov 4;137(43):13736-9. doi: 10.1021/jacs.5b06690.
Tianlu Wang,  Tingting Hong,  Yue Huang 1,  Haomiao Su,  Fan Wu,  Yi Chen,  Lai Wei,  Wei Huang,  Xiaoluan Hua,  Yu Xia,  Jinglei Xu,  Jianhua Gan 2,  Bifeng Yuan,  Yuqi Feng,  Xiaolian Zhang,  Cai-Guang Yang 1,  Xiang Zhou
Affiliations

Affiliations

  • 1 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Shanghai 201203, China.
  • 2 School of Life Sciences, Fudan University , Shanghai 200433, China.
PMID: 26457839 DOI: 10.1021/jacs.5b06690
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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