Xanthine derivatives inhibit FTO in an l -ascorbic acid-dependent manner

Xanthine derivatives were identified as inhibitors of the N 6 -methyladenosine (m6A) demethylase activity of fat-mass-and-obesity-associated protein (FTO) by activity-based high-throughput screening using the m6A-sensitive ribonuclease MazF. Pentoxifylline exhibited l -ascorbic acid concentration-de...

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Published inChemical communications (Cambridge, England) Vol. 59; no. 72; pp. 10809 - 10812
Main Authors Tanaka, Kamui, Suda, Akiyo, Uesugi, Motonari, Futaki, Shiroh, Imanishi, Miki
Format Journal Article
LanguageEnglish
Published Cambridge Royal Society of Chemistry 07.09.2023
Subjects
Ascorbic acid
Inhibitors
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ISSN1359-7345
1364-548X
1364-548X
DOI10.1039/D3CC02484A

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Summary:Xanthine derivatives were identified as inhibitors of the N 6 -methyladenosine (m6A) demethylase activity of fat-mass-and-obesity-associated protein (FTO) by activity-based high-throughput screening using the m6A-sensitive ribonuclease MazF. Pentoxifylline exhibited l -ascorbic acid concentration-dependent inhibitory activity against FTO, an unprecedented mode of inhibition, indicating that l -ascorbic acid is a promising key for designing FTO-specific inhibitors.
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ISSN:1359-7345
1364-548X
1364-548X
DOI:10.1039/D3CC02484A