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Target intelligence / Profile preview
Hypoxia-Inducible Factor 2 (HIF-2)
- Target
- HIF-2
- Molecular classification
- Transcription factor, bHLH-PAS transcription factor
01
Overview
Hypoxia-inducible factor 2 (HIF-2) is a transcription factor that plays a central role in the cellular response to low oxygen levels (hypoxia). It is a heterodimer consisting of an oxygen-sensitive alpha subunit (HIF-2α) and the aryl hydrocarbon receptor nuclear translocator (ARNT). HIF-2 regulates hundreds of genes involved in diverse physiological processes, including erythropoiesis, angiogenesis, and glucose metabolism. Dysregulation of the HIF-2 pathway is implicated in cancer, renal cell carcinoma, and anemia. Drugs targeting HIF-2 are being developed for cancer therapy.
- Other names
- HIF2AHIF-2alphaEPAS1
02
Mechanism of action
Inhibition of HIF-2α heterodimerization with ARNT, blocking transcriptional activation
03
Biological functions
ErythropoiesisAngiogenesisGlucose metabolismCell proliferationCell survivalVascular formation
04
Disease associations
CancerRenal cell carcinomaAnemiaHypoxia-related disorders
05
Safety considerations
Potential for off-target effects due to structural similarity with other HIF isoformsUnpredictable effects on erythropoiesis and angiogenesis in certain contextsPotential for drug resistance development
06
Interacting drugs
Belzutifan
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