Target intelligence / Profile preview

Hypoxia-inducible factor-prolyl hydroxylase (PHD)

Target
PHD
Molecular classification
Enzyme, Oxidoreductase
01

Overview

Hypoxia-inducible factor-prolyl hydroxylases (HIF-PHDs) are a family of iron- and 2-oxoglutarate-dependent enzymes that play a central role in cellular oxygen sensing. They regulate the stability of hypoxia-inducible factors (HIFs), which are transcription factors critical for the cellular response to low oxygen levels (hypoxia). PHD2 is considered the principal oxygen sensor among these isoforms.

Other names
HIF-PHDProlyl hydroxylase domain proteinHIF prolyl-hydroxylaseHypoxia-inducible factor-proline dioxygenaseEGLN1EGLN2EGLN3
02

Mechanism of action

Inhibition of HIF-PHD leads to stabilization and activation of hypoxia-inducible factors (HIFs), even under normoxic conditions.

03

Biological functions

Oxygen sensingRegulation of HIF-alpha stabilityRegulation of erythropoiesisRegulation of angiogenesisRegulation of glycolysisIron metabolism
04

Disease associations

AnemiaChronic kidney diseasePolycythemiaIschemic diseasesPulmonary hypertensionCancer progressionCancer metastasis
05

Safety considerations

Potential for erythrocytosisPossible effects on tumor growth and metastasisEffects on angiogenesis require careful consideration
06

Interacting drugs

HIF prolyl-hydroxylase inhibitors

2 more in the full profile.

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