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

journal_name

ACS Chem Biol

journal_title

ACS chemical biology

authors

Chowdhury R,Candela-Lena JI,Chan MC,Greenald DJ,Yeoh KK,Tian YM,McDonough MA,Tumber A,Rose NR,Conejo-Garcia A,Demetriades M,Mathavan S,Kawamura A,Lee MK,van Eeden F,Pugh CW,Ratcliffe PJ,Schofield CJ

doi

10.1021/cb400088q

subject

Has Abstract

pub_date

2013-07-19 00:00:00

pages

1488-96

issue

7

eissn

1554-8929

issn

1554-8937

journal_volume

8

pub_type

杂志文章

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