Selective small molecule probes for the hypoxia inducible factor (HIF) prolyl hydroxylases.
ACS Chem Biol
; 8(7): 1488-96, 2013 Jul 19.
Article
em En
| MEDLINE
| ID: mdl-23683440
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.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Bibliotecas de Moléculas Pequenas
/
Prolina Dioxigenases do Fator Induzível por Hipóxia
/
Compostos Heterocíclicos
Tipo de estudo:
Prognostic_studies
Limite:
Animals
/
Humans
Idioma:
En
Revista:
ACS Chem Biol
Ano de publicação:
2013
Tipo de documento:
Article
País de afiliação:
Reino Unido