期刊
CHEMICAL COMMUNICATIONS
卷 56, 期 91, 页码 14199-14202出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/d0cc06353c
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资金
- National Natural Science Foundation of China [81973173]
- Jiangsu Province Funds for Excellent Young Scientists [BK20170088]
- Six Talent Peaks Project of Jiangsu Province [YY-023]
- Wellcome Trust [106244/Z/14/Z]
- Cancer Research UK [C9047/A24759]
- BBSRC [BB/R000344/1] Funding Source: UKRI
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.
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