Selective small molecule probes for the hypoxia inducible factor (HIF) Prolyl Hydroxylases

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Title
Selective small molecule probes for the hypoxia inducible factor (HIF) Prolyl Hydroxylases
Author(s)
R Chowdhury; J I Candela-Lena; M C Chan; D J Greenald; K K Yeoh; Y M Tian; M A McDonough; A Tumber; N R Rose; A Conejo-Garcia; M Demetriades; S Mathavan; A Kawamura; Myung Kyu Lee; F Eeden; C W Pugh; P J Ratcliffe; C J Schofield
Bibliographic Citation
ACS Chemical Biology, vol. 8, no. 7, pp. 1488-1496
Publication Year
2013
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.
ISSN
1554-8929
Publisher
Amer Chem Soc
DOI
http://dx.doi.org/10.1021/cb400088q
Type
Article
Appears in Collections:
1. Journal Articles > Journal Articles
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