Target intelligence / Profile preview

Hypoxia-Inducible Factor (None)

Target
None
Molecular classification
Transcription factor, bHLH-PAS protein
01

Overview

Hypoxia-inducible factors (HIFs) are a family of transcription factors that play a central role in cellular adaptation to low oxygen (hypoxic) conditions. They regulate the expression of genes involved in processes such as angiogenesis, erythropoiesis, metabolism, and cell survival under hypoxic stress. HIFs function as heterodimers composed of an oxygen-sensitive alpha subunit (HIF-1α, HIF-2α, and HIF-3α) and a constitutively expressed beta subunit (ARNT). Under normoxia, the alpha subunit is hydroxylated, leading to its degradation. Under hypoxia, hydroxylation is inhibited, the alpha subunit stabilizes, dimerizes with the beta subunit, and activates transcription of target genes.

Other names
HIFHIF-1HIF-1alphaHIF-2alphaHIF-3alphaARNTHIF-1betaAryl Hydrocarbon Receptor Nuclear Translocator
02

Mechanism of action

Inhibition of HIF prolyl hydroxylation, disruption of HIF-VHL interaction, inhibition of HIF transcriptional activity

03

Biological functions

Regulation of gene expressionResponse to hypoxiaAngiogenesisErythropoiesisMetabolic adaptationCell survivalCell proliferation
04

Disease associations

CancerIschemic diseasesTumorigenesisMetabolic disorders
05

Safety considerations

Off-target effects of HIF inhibitorsPotential for disrupting normal physiological responses to hypoxia
06

Interacting drugs

PHD inhibitors

1 more in the full profile.

07

Biomarkers

HIF-1alpha expressionVEGF expression

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