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
- Full Text Link
- http://dx.doi.org/10.1021/cb400088q
- Type
- Article
- Appears in Collections:
- 1. Journal Articles > Journal Articles
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