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A small-molecule probe for monitoring binding to prolyl hydroxylase domain 2 by fluorescence polarisation

Abstract:
Inhibition of the dioxygen sensing hypoxia-inducible factor prolyl hydroxylases has potential therapeutic benefit for treatment of diseases, including anaemia. We describe the discovery of a small-molecule probe useful for monitoring binding to human prolyl hydroxylase domain 2 (PHD2) via fluorescence polarisation. The assay is suitable for high-throughput screening of PHD inhibitors with both weak and strong affinities, as shown by work with clinically used inhibitors and naturally occurring PHD inhibitors.
Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1039/D0CC06353C

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Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Role:
Author
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Publisher:
Royal Society of Chemistry Publisher's website
Journal:
Chemical Communications Journal website
Volume:
56
Issue:
2020
Pages:
14199-14202
Publication date:
2020-10-23
Acceptance date:
2020-10-20
DOI:
EISSN:
1364-548X
ISSN:
1359-7345
Language:
English
Keywords:
Pubs id:
1138604
Local pid:
pubs:1138604
Deposit date:
2020-10-21

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