Target intelligence / Profile preview

Hypoxia-inducible factor 1-alpha (HIF-1α)

Target
HIF-1α
Molecular classification
Transcription factor, Basic helix-loop-helix PAS domain-containing protein
01

Overview

Hypoxia-inducible factor 1-alpha (HIF-1α) is a subunit of the heterodimeric transcription factor hypoxia-inducible factor 1 (HIF-1), encoded by the HIF1A gene. It is considered the master regulator of cellular and developmental responses to hypoxia, or low oxygen conditions. HIF-1α plays a central role in regulating genes involved in angiogenesis, energy metabolism, cell survival, tumor invasion, and vascularization.

Other names
HIF1A
02

Mechanism of action

Currently under research. Several compounds are being developed to inhibit HIF-1α or its downstream targets, aiming to disrupt the pathways that promote tumor growth, angiogenesis, and metastasis. Inhibition typically involves destabilizing HIF-1α, interfering with its dimerization with ARNT/HIF-1β, or blocking its ability to bind to hypoxia-responsive elements (HREs).

03

Biological functions

AngiogenesisGlycolysisCell survivalEmbryonic developmentVascularizationRegulation of gene expression in response to hypoxia
04

Disease associations

CancerIschemic diseasesMetabolic disorders
05

Safety considerations

Potential for off-target effects due to the broad range of HIF-1α target genesDisruption of normal physiological responses to hypoxia
06

Biomarkers

HIF-1α expression levels in tumor tissue

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