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Potent and selective triazole-based inhibitors of the hypoxia-inducible factor prolyl-hydroxylases with activity in the murine brain

Abstract:

As part of the cellular adaptation to limiting oxygen availability in animals, the expression of a large set of genes is activated by the upregulation of the hypoxia-inducible transcription factors (HIFs). Therapeutic activation of the natural human hypoxic response can be achieved by the inhibition of the hypoxia sensors for the HIF system, i.e. the HIF prolyl-hydroxylases (PHDs). Here, we report studies on tricyclic triazole-containing compounds as potent and selective PHD inhibitors which ...

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Publication status:
Published
Peer review status:
Peer reviewed

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Publisher copy:
10.1371/journal.pone.0132004

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Institution:
University of Oxford
Division:
MSD
Department:
NDM
Sub department:
CCMP
Role:
Author
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Funding agency for:
Schofield, C
Grant:
PG/12/33/29546
More from this funder
Funding agency for:
Schofield, C
Grant:
PG/12/33/29546
Publisher:
Public Library of Science Publisher's website
Journal:
PloS one Journal website
Volume:
10
Issue:
7
Pages:
e0132004
Publication date:
2015-01-01
Acceptance date:
2015-06-09
DOI:
EISSN:
1932-6203
ISSN:
1932-6203
Source identifiers:
531099
Language:
English
Pubs id:
pubs:531099
UUID:
uuid:2139f408-d035-4e8d-8f27-2a2cf58fb3f1
Local pid:
pubs:531099
Deposit date:
2016-03-22

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