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Structure-based design of selective fat mass and obesity associated protein (FTO) inhibitors

Abstract:

FTO catalyzes the Fe(II) and 2-oxoglutarate (2OG)-dependent modification of nucleic acids, including the demethylation of N6-methyladenosine (m6A) in mRNA. FTO is a proposed target for anti-cancer therapy. Using information from crystal structures of FTO in complex with 2OG and substrate mimics, we designed and synthesized two series of FTO inhibitors, which were characterized by turnover and binding assays, and by X-ray crystallography with FTO and the related bacterial enzyme AlkB. A potent...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher:
American Chemical Society Publisher's website
Journal:
Journal of Medicinal Chemistry Journal website
Volume:
64
Issue:
22
Pages:
16609-16625
Publication date:
2021-11-11
Acceptance date:
2021-11-11
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
Pmid:
34762429
Language:
English
Keywords:
Pubs id:
1210808
Local pid:
pubs:1210808
Deposit date:
2022-01-10

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