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ACS Chem Biol. 2013 Jul 19;8(7):1488-96. doi: 10.1021/cb400088q. Epub 2013 Jun 12.

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

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  • 1Department of Chemistry, Chemistry Research Laboratory, University of Oxford , Mansfield Road, Oxford, OX1 3TA, United Kingdom.

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 oxygenases. We identify suitable probe compounds for use in studies on the functional effects of PHD inhibition in cells and in animals.

PMID:
23683440
DOI:
10.1021/cb400088q
[PubMed - indexed for MEDLINE]
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