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2-Oxoglutarate derivatives can selectively enhance or inhibit the activity of human oxygenases

Abstract:

2-Oxoglutarate (2OG) oxygenases are validated agrochemical and human drug targets. The potential for modulating their activity with 2OG derivatives has not been explored, possibly due to concerns regarding selectivity. We report proof-of-principle studies demonstrating selective enhancement or inhibition of 2OG oxygenase activity by 2-oxo acids. The human 2OG oxygenases studied, factor inhibiting hypoxia-inducible transcription factor HIF-α (FIH) and aspartate/asparagine-β-hydroxylase (AspH),...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1038/s41467-021-26673-2

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Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
ORCID:
0000-0002-0290-6565
Publisher:
Springer Nature Publisher's website
Journal:
Nature Communications Journal website
Volume:
12
Article number:
6478
Publication date:
2021-11-10
Acceptance date:
2021-10-12
DOI:
EISSN:
2041-1723
Language:
English
Keywords:
Pubs id:
1200953
Local pid:
pubs:1200953
Deposit date:
2021-10-12

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