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Discovery of neuroprotective agents that inhibit human prolyl hydroxylase PHD2

Abstract:

Prolyl hydroxylase (PHD) enzymes play a critical role in the cellular responses to hypoxia through their regulation of the hypoxia inducible factor α (HIF-α) transcription factors. PHD inhibitors show promise for the treatment of diseases including anaemia, cardiovascular disease and stroke. In this work, a pharmacophore-based virtual high throughput screen was used to identify novel potential inhibitors of human PHD2. Two moderately potent new inhibitors were discovered, with IC50 values of ...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1016/j.bmc.2021.116115

Authors


More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
More by this author
Institution:
University of Oxford
Division:
MPLS
Department:
Chemistry
Sub department:
Organic Chemistry
Role:
Author
ORCID:
0000-0002-0290-6565
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Publisher:
Elsevier Publisher's website
Journal:
Bioorganic and Medicinal Chemistry Journal website
Volume:
38
Article number:
116115
Publication date:
2021-03-24
Acceptance date:
2021-03-13
DOI:
ISSN:
0968-0896
Language:
English
Keywords:
Pubs id:
1169353
Local pid:
pubs:1169353
Deposit date:
2021-03-26

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