Assay for glutathiane transferase using polyhaloaryl-substituted
申请人:Molecule Probes, Inc.
公开号:US05773236A1
公开(公告)日:1998-06-30
The subject invention describes compounds containing a polyhalogenated aryl moiety. The compounds of the invention are particularly useful for the assay of a variety of enzymes, including intracellular enzymes. The subject invention also describes assays for glutathione and/or glutathione transferase enzymes. Selected compounds of the invention are particularly useful for improving the retention of fluorescent products of enzyme metabolism in cells.
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.