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Selective small molecule probes for the hypoxia inducible factor (HIF) prolyl hydroxylases.

Abstract:

The hypoxia inducible factor (HIF) system is central to the signaling of low oxygen (hypoxia) in animals. The levels of HIF-α isoforms are regulated in an oxygen-dependent manner by the activity of the HIF prolyl-hydroxylases (PHD or EGLN enzymes), which are Fe(II) and 2-oxoglutarate (2OG) dependent oxygenases. Here, we describe biochemical, crystallographic, cellular profiling, and animal studies on PHD inhibitors including selectivity studies using a representative set of human 2OG oxygenas...

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Publication status:
Published

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Publisher copy:
10.1021/cb400088q

Authors


Chowdhury, R More by this author
Candela-Lena, JI More by this author
Greenald, DJ More by this author
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Journal:
ACS chemical biology
Volume:
8
Issue:
7
Pages:
1488-1496
Publication date:
2013-07-05
DOI:
EISSN:
1554-8937
ISSN:
1554-8929
URN:
uuid:d34b8ca7-7b8b-401d-8263-162828c03d96
Source identifiers:
401563
Local pid:
pubs:401563

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