| Literature DB >> 23683440 |
Rasheduzzaman Chowdhury1, José Ignacio Candela-Lena, Mun Chiang Chan, David Jeremy Greenald, Kar Kheng Yeoh, Ya-Min Tian, Michael A McDonough, Anthony Tumber, Nathan R Rose, Ana Conejo-Garcia, Marina Demetriades, Sinnakaruppan Mathavan, Akane Kawamura, Myung Kyu Lee, Freek van Eeden, Christopher W Pugh, Peter J Ratcliffe, Christopher J Schofield.
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.Entities:
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Year: 2013 PMID： 23683440 DOI： 10.1021/cb400088q
Source DB: PubMed Journal: ACS Chem Biol ISSN： 1554-8929 Impact factor: 5.100