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

Yu Nakashima; Lennart Brewitz; Anthony Tumber; Eidarus Salah; Christopher J. Schofield

doi:10.1038/s41467-021-26673-2

Nature Communications (Nov 2021)

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

Yu Nakashima,
Lennart Brewitz,
Anthony Tumber,
Eidarus Salah,
Christopher J. Schofield

Affiliations

Yu Nakashima: Chemistry Research Laboratory, Department of Chemistry and the Ineos Oxford Institute for Antimicrobial Research, University of Oxford
Lennart Brewitz: Chemistry Research Laboratory, Department of Chemistry and the Ineos Oxford Institute for Antimicrobial Research, University of Oxford
Anthony Tumber: Chemistry Research Laboratory, Department of Chemistry and the Ineos Oxford Institute for Antimicrobial Research, University of Oxford
Eidarus Salah: Chemistry Research Laboratory, Department of Chemistry and the Ineos Oxford Institute for Antimicrobial Research, University of Oxford
Christopher J. Schofield: Chemistry Research Laboratory, Department of Chemistry and the Ineos Oxford Institute for Antimicrobial Research, University of Oxford

DOI: https://doi.org/10.1038/s41467-021-26673-2
Journal volume & issue: Vol. 12, no. 1
pp. 1 – 17

Abstract

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The human 2-oxoglutarate (2OG) oxygenases FIH and AspH are relevant drug targets. Here, the authors show that synthetic and naturally occurring 2OG derivatives can selectively modulate FIH and AspH activities, suggesting that these compounds may serve as a basis to develop 2OG oxygenase-targeting probes and drugs.

Published in Nature Communications

ISSN: 2041-1723 (Online)
Publisher: Nature Portfolio
Country of publisher: United Kingdom
LCC subjects: Science
Website: https://www.nature.com/ncomms/

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